TECHNICAL FIELD

The present invention belongs to the field of chemistry, and particularly relates to a substituted pyrimidine compound and a preparation method and use thereof as a fungicide, an insecticide and an acaricide.

BACKGROUND

Patent WO9507278 published the general formulas of pyrimidine-containing substituted pyrazole compounds as shown in the following general formulas and the application of specific compounds CK1 and CK2 as an agricultural fungicide, an insecticide and an acaricide.



The following compounds CK3, CK4 and CK5 were searched online through Scifinder, but no reference was found.



However, the substituted pyrimidine compound having the structure shown by the general formula I of the present invention had not been reported.

SUMMARY

The purpose of the present invention is to provide a pyrimidine-containing substituted pyrazole compound capable of controlling various fungi, pests and mites, and a preparation method and use thereof for preparing medicine for controlling fungi, pests and mites in agriculture or other fields.

To achieve the above purpose, the present invention adopts the following technical solution:

The present invention provides a substituted pyrimidine compound. The substituted pyrimidine compound is a compound shown by general formula I:



in the formula:

R1is selected from hydrogen, halogen, cyano, nitro, amino, carboxyl, C1-C12alkyl, halogenated C1-C12alkyl, C3-C12cycloalkyl, C1-C12alkoxy, halogenated C1-C12alkoxy, C1-C12alkylthio, halogenated C1-C12alkylthio, C1-C12alkylsulfinyl, C1-C12alkylsulfonyl, C2-C12alkenyl, halogenated C2-C12alkenyl, C2-C12alkynyl, halogenated C2-C12alkynyl, C3-C12alkenyloxy, halogenated C3-C12alkenyloxy, C3-C12alkynyloxy, halogenated C3-C12alkynyloxy, C1-C12alkylamino, di(C1-C12alkyl)amino, C1-C12alkylaminocarbonyl, halogenated C1-C12alkylaminocarbonyl, C1-C12alkoxycarbonyl, halogenated C1-C12alkoxycarbonyl, C1-C12alkoxy C1-C12alkyl or C1-C12alkylthio C1-C12alkyl;

R2is selected from hydrogen, halogen, cyano, nitro, amino, carboxyl, formyl, C1-C12alkyl, halogenated C1-C12alkyl, C1-C12alkoxy or halogenated C1-C12alkoxy;

R1and R2can also form a five-membered ring, six-membered ring, seven-membered ring or eight-membered ring containing C, N, O or S together with a connected pyrimidine ring;

X is selected from NR3, O or S;

R3is selected from hydrogen, hydroxyl, formyl, C1-C12alkyl, halogenated C1-C12alkyl, C1-C12alkoxyl, halogenated C1-C12alkoxyl, C3-C12cycloalkyl, C1-C12alkylthio, C2-C12alkenylthio, C2-C12alkenyl, C2-C12alkynyl, halogenated C2-C12alkenyl, halogenated C2-C12alkynyl, C1-C12alkoxy C1-C12alkyl, halogenated C1-C12alkoxy C1-C12alkyl, C1-C12alkylthio C1-C12alkyl, halogenated C1-C12alkylthio C1-C12alkyl, C1-C12alkylsulfinyl, halogenated C1-C12alkylsulfinyl, C1-C12alkylsulfonyl, halogenated C1-C12alkylsulfonyl, C1-C12alkylaminosulfonyl, di(C1-C12alkyl) aminosulfonyl, C1-C12alkylsulfonylaminocarbonyl, C1-C12alkylcarbonylaminosulfonyl, C3-C12cycloalkyloxycarbonyl, C1-C12alkylcarbonyl, halogenated C1-C12alkylcarbonyl, C1-C12alkoxycarbonyl, halogenated C1-C12alkoxycarbonyl, C1-C12alkylcarbonyl C1-C12alkyl, C1-C12alkoxycarbonyl C1-C12alkyl, C1-C12alkylaminocarbonyl, di(C1-C12alkyl)aminocarbonyl, C2-C12alkenyloxycarbonyl, C2-C12alkynyloxycarbonyl, C1-C12alkoxy C1-C12alkoxycarbonyl, C1-C12alkylaminothio, di(C1-C12alkyl)aminothio, and unsubstituted or substituted arylcarbonyl C1-C6alkyl, arylcarbonyl, aryloxycarbonyl, aryl C1-C6alkyloxycarbonyl, aryl C1-C6alkyl, heteroarylcarbonyl C1-C6alkyl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroaryl C1-C6alkyloxycarbonyl and heteroaryl C1-C6alkyl by 1-5 of the following groups, the following groups are halogen, nitro, cyano, C1-C6alkyl, halogenated C1-C6alkyl, C1-C6alkoxy or halogenated C1-C6alkoxy;

R4and R5are the same or different, and are respectively selected from hydrogen, halogen, C1-C12alkyl, halogenated C1-C12alkyl, C1-C12alkoxyl or halogenated C1-C12alkoxyl,

wherein R4and R5can also form a C3-C8ring together with the connected C;

R6and R7are the same or different, and are respectively selected from hydrogen, halogen, C1-C12alkyl, halogenated C1-C12alkyl, C1-C12alkoxyl or halogenated C1-C12alkoxyl,

wherein R6and R7can also form a C3-C8ring together with the connected C;

m is selected from an integer from 0 to 5;

R8is selected from hydrogen, cyano, halogen, C1-C12alkyl, halogenated C1-C12alkyl, C1-C12alkoxycarbonyl, halogenated C1-C12alkoxycarbonyl, and unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

R9is selected from hydrogen, C1-C12alkyl, C3-C8cycloalkyl, halogenated C1-C12alkyl, C1-C12alkylcarbonyl, halogenated C1-C12alkylcarbonyl, C1-C12alkylsulfonyl, halogenated C1-C12alkylsulfonyl, C1-C12alkoxycarbonyl, C1-C12alkoxy C1-C12alkyl, C1-C12alkoxycarbonyl C1-C12alkyl, and unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

R10is selected from halogen, hydroxyl, amino, cyano, nitro, C1-C12alkyl, halogenated C1-C12alkyl, C1-C12alkoxy, halogenated C1-C12alkoxy, C1-C12cycloalkyl, C1-C12alkylamino, halogenated C1-C12alkylamino, di(C1-C12alkyl)amino, halogenated di(C1-C12alkyl)amino, C(═O)NR11R12, C1-C12alkylthio, halogenated C1-C12alkylthio, C2-C12alkenyl, C2-C12alkynyl, C2-C12alkenyloxy, halogenated C2-C12alkenyloxy, C2-C12alkynyloxy, halogenated C2-C12alkynyloxy, C1-C12alkylsulfonyl, halogenated C1-C12alkylsulfonyl, C1-C12alkylcarbonyl, halogenated C1-C12alkylcarbonyl, C1-C12alkoxycarbonyl, halogenated C1-C12alkoxycarbonyl, C1-C12alkoxy C1-C12alkyl, halogenated C1-C12alkoxy C1-C12alkyl, C1-C12alkylthio C1-C12alkyl, halogenated C1-C12alkylthio C1-C12alkyl, C1-C12alkoxycarbonyl C1-C12alkyl, halogenated C1-C12alkoxycarbonyl C1-C12alkyl, C1-C12alkylthiocarbonyl C1-C12alkyl, halogenated C1-C12alkylthiocarbonyl C1-C12alkyl, C1-C12alkylcarbonyloxy, halogenated C1-C12alkylcarbonyloxy, C1-C12alkoxycarbonyloxy, halogenated C1-C12alkoxycarbonyloxy, C1-C12alkylsulfonyloxy, halogenated C1-C12alkylsulfonyloxy, C1-C12alkoxy C1-C12alkoxyl or halogenated C1-C12alkoxy C1-C12alkoxyl;

R11and R12are the same or different, and are respectively selected from hydrogen, C1-C12alkyl or halogenated C1-C12alkyl;

W is selected from hydrogen, halogen, C1-C12alkyl, halogenated C1-C12alkyl, C3-C8cycloalkyl, C1-C12alkoxyl, C1-C12alkylthio or C1-C12alkylsulfonyl;

Q is selected from unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

or salt of the compound shown by the general formula I.

In the substituted pyrimidine compound of the present invention, an optional compound comprises: in the general formula I:

R1is selected from hydrogen, halogen, cyano, nitro, amino, carboxyl, C1-C6alkyl, halogenated C1-C6alkyl, C3-C6cycloalkyl, C1-C6alkoxy, halogenated C1-C6alkoxyl, C1-C6alkylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, halogenated C1-C6alkylthio, C2-C6alkenyl, halogenated C2-C6alkenyl, C2-C6alkynyl, halogenated C2-C6alkynyl, C3-C6alkenyloxy, halogenated C3-C6alkenyloxy, C3-C6alkynyloxy, halogenated C3-C6alkynyloxy, C1-C6Alkylamino, di(C1-C6alkyl) amino, C1-C6alkylaminocarbonyl, halogenated C1-C6alkylaminocarbonyl, C1-C6alkoxycarbonyl, halogenated C1-C6alkoxycarbonyl, C1-C6alkoxy C1-C6alkyl or C1-C6alkylthio C1-C6alkyl;

R2is selected from hydrogen, halogen, cyano, nitro, amino, carboxyl, formyl, C1-C6alkyl, halogenated C1-C6alkyl, C1-C6alkoxy or halogenated C1-C6alkoxy;

R1and R2can also form a five-membered ring or six-membered ring containing C, N, O or S together with a connected pyrimidine ring;

X is selected from NR3, O or S;

R3is selected from hydrogen, hydroxyl, formyl, C1-C6alkyl, halogenated C1-C6alkyl, C1-C6alkoxy, halogenated C1-C6alkoxyl, C3-C6cycloalkyl, C1-C6alkylthio, C2-C6alkenylthio, C2-C6alkenyl, C2-C6alkynyl, halogenated C2-C6alkenyl, halogenated C2-C6alkynyl, C1-C6alkoxy C1-C6alkyl, halogenated C1-C6alkoxy C1-C6alkyl, C1-C6alkylthio C1-C6alkyl, halogenated C1-C6alkylthio C1-C6alkyl, C1-C6alkylsulfinyl, halogenated C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, halogenated C1-C6alkylsulfonyl, C1-C6alkylaminosulfonyl, di(C1-C6alkyl) aminosulfonyl, C1-C6alkylsulfonylaminocarbonyl, C1-C6alkylcarbonylaminosulfonyl, C2-C6cycloalkyloxycarbonyl, C1-C6alkylcarbonyl, halogenated C1-C6alkylcarbonyl, C1-C6alkoxycarbonyl, halogenated C1-C6alkoxycarbonyl, C1-C6alkylcarbonyl C1-C6alkyl, C1-C6alkoxycarbonyl C1-C6alkyl, C1-C6alkylaminocarbonyl, di(C1-C6alkyl) aminocarbonyl, C2-C6alkenyloxycarbonyl, C2-C6alkynyloxycarbonyl, C1-C6alkoxy C1-C6alkoxycarbonyl, C1-C6alkylaminothio, di(C1-C6alkyl) aminothio, and unsubstituted or substituted arylcarbonyl C1-C6alkyl, arylcarbonyl, aryloxycarbonyl, aryl C1-C6alkyloxycarbonyl, aryl C1-C6alkyl, heteroarylcarbonyl C1-C6alkyl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroaryl C1-C6alkyloxycarbonyl and heteroaryl C1-C6alkyl by 1-5 of the following groups, the following groups are halogen, nitro, cyano, C1-C6alkyl, halogenated C1-C6alkyl, C1-C6alkoxy or halogenated C1-C6alkoxy;

R4and R5are the same or different, and are respectively selected from hydrogen, halogen, C1-C6alkyl, halogenated C1-C6alkyl, C1-C6alkoxy or halogenated C1-C6alkoxy;

wherein R4and R5can also form a C3-C6ring together with the connected C;

R6and R7are the same or different, and are respectively selected from hydrogen, halogen, C1-C6alkyl, halogenated C1-C6alkyl, C1-C6alkoxyl or halogenated C1-C6alkoxyl;

wherein R6and R7can also form a C3-C6ring together with the connected C;

m is selected from an integer from 0 to 4;

R8is selected from hydrogen, cyano, halogen, C1-C6alkyl, halogenated C1-C6alkyl, C1-C6alkoxycarbonyl, halogenated C1-C6alkoxycarbonyl, and unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

R9is selected from hydrogen, C1-C6alkyl, C3-C6cycloalkyl, halogenated C1-C6alkyl, C1-C6alkylcarbonyl, halogenated Q-C6alkylcarbonyl, C1-C6alkylsulfonyl, halogenated C1-C6alkylsulfonyl, C1-C6alkoxycarbonyl, C1-C6alkoxy C1-C6alkyl, C1-C6alkoxycarbonyl C1-C6alkyl, and unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

R10is selected from halogen, hydroxyl, amino, cyano, nitro, C1-C6alkyl, halogenated C1-C6alkyl, C1-C6alkoxyl, halogenated C1-C6alkoxy, C3-C6cycloalkyl, C1-C6alkylamino, halogenated C1-C6alkylamino, di(C1-C6alkyl) amino, halogenated di(C1-C6alkyl) amino, C(═O)NR11R12, C1-C6alkylthio, halogenated C1-C6alkylthio, C2-C6alkenyl, C2-C6alkynyl, C2-C6alkenyloxy, halogenated C2-C6alkenyloxy, C2-C6alkynyloxy, halogenated C2-C6alkynyloxy, C1-C6alkylsulfonyl, halogenated C1-C6alkylsulfonyl, C1-C6alkylcarbonyl, halogenated C1-C6alkylcarbonyl, C1-C6alkoxycarbonyl, halogenated C1-C6alkoxycarbonyl, C1-C6alkoxy C1-C6alkyl, halogenated C1-C6alkoxy C1-C6alkyl, C1-C6alkylthio C1-C6alkyl, halogenated C1-C6alkylthio C1-C6alkyl, C1-C6alkoxycarbonyl C1-C6alkyl, halogenated C1-C6alkoxycarbonyl C1-C6alkyl, C1-C6alkylthiocarbonyl C1-C6alkyl, halogenated C1-C6alkylthiocarbonyl C1-C6alkyl, C1-C6alkylcarbonyloxy, halogenated C1-C6alkylcarbonyloxy, C1-C6alkoxycarbonyloxy, halogenated C1-C6alkoxycarbonyloxy, C1-C6alkylsulfonyloxy, halogenated C1-C6alkylsulfonyloxy, C1-C6alkoxy C1-C6alkoxy or halogenated C1-C6alkoxy C1-C6alkoxy;

R11and R12are the same or different, and are respectively selected from hydrogen, C1-C12alkyl or halogenated C1-C12alkyl;

W is selected from hydrogen, halogen, C1-C6alkyl, halogenated C1-C6alkyl, C3-C6cycloalkyl, C1-C6alkoxy, C1-C6alkylthio or C1-C6alkylsulfonyl;

Q is selected from unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

or salt of the compound shown by the general formula I.

In the substituted pyrimidine compound of the present invention, a relatively optional compound comprises: in the general formula I, Q is selected from aryl unsubstituted or substituted by one to five R10; the structural formula of the general formula I of the compound is further shown by I-1:



in the formula,

R1is selected from hydrogen, halogen, cyano, nitro, amino, carboxyl, C1-C4alkyl, halogenated C1-C4alkyl, C3-C4cycloalkyl, C1-C4alkoxyl, halogenated C1-C4alkoxyl, C1-C4alkylthio, C1-C4alkylsulfinyl, C1-C4alkylsulfonyl, halogenated C1-C4alkylthio, C2-C4alkenyl, halogenated C2-C4alkenyl, C2-C4alkynyl, halogenated C2-C4alkynyl, C3-C4alkenyloxy, halogenated C3-C4alkenyloxy, C3-C4alkynyloxy, halogenated C3-C4alkynyloxy, C1-C4alkylamino, di(C1-C4alkyl) amino, C1-C4alkylaminocarbonyl, halogenated C1-C4alkylaminocarbonyl, C1-C4alkoxycarbonyl, halogenated C1-C4alkoxycarbonyl, C1-C4alkoxy C1-C4alkyl or C1-C4alkylthio C1-C4alkyl;

R2is selected from hydrogen, halogen, cyano, nitro, amino, carboxyl, formyl, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkox, or halogenated C1-C4alkoxyl;

R1and R2can also form a five-membered ring or six-membered ring containing C, N, O or S together with a connected pyrimidine ring;

X is selected from NR3, O or S;

R3is selected from hydrogen, hydroxyl, formyl, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxy, halogenated C1-C4alkoxy, C3-C4cycloalkyl, C1-C4alkylthio, C2-C4alkenylthio, C2-C4alkenyl, C2-C4alkynyl, halogenated C2-C4alkenyl, halogenated C2-C4alkynyl, C1-C4alkoxy C1-C4alkyl, halogenated C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, halogenated C1-C4alkylthio C1-C4alkyl, C1-C4alkylsulfinyl, halogenated C1-C4alkylsulfinyl, C1-C4alkylsulfonyl, halogenated C1-C4alkylsulfonyl, C1-C4alkylaminosulfonyl, di(C1-C4alkyl) aminosulfonyl, C1-C4alkylsulfonylaminocarbonyl, C1-C4alkylcarbonylaminosulfonyl, C3-C4cycloalkyloxycarbonyl, C1-C4alkylcarbonyl, halogenated C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, halogenated C1-C4alkoxycarbonyl, C1-C4alkylcarbonyl C1-C4alkyl, C1-C4alkoxycarbonyl C1-C4alkyl, C1-C4alkylaminocarbonyl, di(C1-C4alkyl) aminocarbonyl, C2-C4alkenyloxycarbonyl, C2-C4alkynyloxycarbonyl, C1-C4alkoxy C1-C4alkoxycarbonyl, C1-C4alkylaminothio, di(C1-C4alkyl) aminothio, and unsubstituted or substituted arylcarbonyl C1-C4alkyl, arylcarbonyl, aryloxycarbonyl, aryl C1-C4alkyloxycarbonyl, aryl C1-C4alkyl, heteroarylcarbonyl C1-C4alkyl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroaryl C1-C4alkyloxycarbonyl and heteroaryl C1-C4alkyl by 1-5 of the following groups, the following groups are halogen, nitro, cyano, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxy or halogenated C1-C6alkoxy;

R4and R5are the same or different, and are respectively selected from hydrogen, halogen, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxy or halogenated C1-C4alkoxy;

wherein R4and R5can also form a C3-C4ring together with the connected C;

R6and R7are the same or different, and are respectively selected from hydrogen, halogen, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxyl or halogenated C1-C4alkoxyl;

wherein R6and R7can also form a C3-C4ring together with the connected C;

m is selected from an integer from 0 to 3;

R8is selected from hydrogen, cyano, halogen, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxycarbonyl, halogenated C1-C4alkoxycarbonyl, and unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

R9is selected from hydrogen, C1-C4alkyl, C3-C4cycloalkyl, halogenated C1-C4alkyl, C1-C4alkylcarbonyl, halogenated C1-C4alkylcarbonyl, C1-C4alkylsulfonyl, halogenated C1-C4alkylsulfonyl, C1-C4alkoxycarbonyl, C1-C4alkoxy C1-C4alkyl, C1-C4alkoxycarbonyl C1-C4alkyl, and unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

R10is selected from halogen, hydroxyl, amino, cyano, nitro, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxyl, halogenated C1-C4alkoxy, C3-C4cycloalkyl, C1-C4alkylamino, halogenated C1-C4alkylamino, di(C1-C4alkyl) amino, halogenated di(C1-C4alkyl) amino, C(═O)NR12R13, C1-C4alkylthio, halogenated C1-C4alkylthio, C2-C4alkenyl, C2-C4alkynyl, C2-C4alkenyloxy, halogenated C2-C4alkenyloxy, C2-C4alkynyloxy, halogenated C2-C4alkynyloxy, C1-C4alkylsulfonyl, halogenated C1-C4alkylsulfonyl, C1-C4alkylcarbonyl, halogenated C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, halogenated C1-C4alkoxycarbonyl, C1-C4alkoxy C1-C4alkyl, halogenated C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, halogenated C1-C4alkylthio C1-C4alkyl, C1-C4alkoxycarbonyl C1-C4alkyl, halogenated C1-C4alkoxycarbonyl C1-C4alkyl, C1-C4alkylthiocarbonyl C1-C4alkyl, halogenated C1-C4alkylthiocarbonyl C1-C4alkyl, C1-C4alkylcarbonyloxy, halogenated C1-C4alkylcarbonyloxy, C1-C4alkoxycarbonyloxy, halogenated C1-C4alkoxycarbonyloxy, C1-C4alkylsulfonyloxy, halogenated C1-C4alkylsulfonyloxy, C1-C4alkoxy C1-C4alkoxy or halogenated C1-C4alkoxy C1-C4alkoxy;

R11and R12are the same or different, and are respectively selected from hydrogen, C1-C12alkyl or halogenated C1-C12alkyl;

W is selected from hydrogen, halogen, C1-C4alkyl, halogenated C1-C4alkyl, C3-C4cycloalkyl, C1-C4alkoxy, C1-C4alkylthio or C1-C4alkylsulfonyl;

or salt formed by the compound shown by general formula I-1 and hydrochloric acid, sulfuric acid, phosphoric acid, formic acid, acetic acid, trifluoroacetic acid, oxalic acid, methanesulfonic acid, p-toluenesulfonic acid, benzoic acid, phthalic acid, maleic acid, fumaric acid, sorbic acid, malic acid or citric acid.

In the substituted pyrimidine compound of the present invention, a further optional compound comprises: the structure of the compound shown by the general formula I-1 is: I-1A, I-1B, I-1C and I-1D;



in the formula:

R4and R5are the same or different, and are respectively selected from hydrogen, halogen, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxyl or halogenated C1-C4alkoxyl;

wherein R4and R5can also form a C3-C4ring together with the connected C;

R6and R7are the same or different, and are respectively selected from hydrogen, halogen, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxyl or halogenated C1-C4alkoxyl;

wherein R6and R7can also form a C3-C4ring together with the connected C;

m is selected from an integer from 0 to 3;

R8and R9are the same or different, and are respectively selected from hydrogen, cyano, halogen, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxycarbonyl, halogenated C1-C4alkoxycarbonyl, and unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

R10is selected from halogen, hydroxyl, amino, cyano, nitro, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxyl, halogenated C1-C4alkoxy, C3-C4cycloalkyl, C1-C4alkylamino, halogenated C1-C4alkylamino, di(C1-C4alkyl) amino, halogenated di(C1-C4alkyl) amino, C(═O)NR11R12, C1-C4alkylthio, halogenated C1-C4alkylthio, C2-C4alkenyl, C2-C4alkynyl, C2-C4alkenyloxy, halogenated C1-C4alkenyloxy, C1-C4alkynyloxy, halogenated C2-C4alkynyloxy, C1-C4alkylsulfonyl, halogenated C1-C4alkylsulfonyl, C1-C4alkylcarbonyl, halogenated C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, halogenated C1-C4alkoxycarbonyl, C1-C4alkoxy C1-C4alkyl, halogenated C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, halogenated C1-C4alkylthio C1-C4alkyl, C1-C4alkoxycarbonyl C1-C4alkyl, halogenated C1-C4alkoxycarbonyl C1-C4alkyl, C1-C4alkylthiocarbonyl C1-C4alkyl, halogenated C1-C4alkylthiocarbonyl C1-C4alkyl, C1-C4alkylcarbonyloxy, halogenated C1-C4alkylcarbonyloxy, C1-C4alkoxycarbonyloxy, halogenated C1-C4alkoxycarbonyloxy, C1-C4alkylsulfonyloxy, halogenated C1-C4alkylsulfonyloxy, C1-C4alkoxy C1-C4alkoxy or halogenated C1-C4alkoxy C1-C4alkoxy;

n is selected from an integer from 0 to 5; when n is 0, a benzene ring has no substituent; when n is greater than 1, R10is the same or different;

R11and R12are the same or different and are respectively selected from hydrogen, C1-C4alkyl or halogenated C1-C4alkyl;

W is selected from hydrogen, halogen, C1-C4alkyl, halogenated C1-C4alkyl, C3-C4cycloalkyl, C1-C4alkoxy, C1-C4alkylthio or C1-C4alkylsulfonyl;

moreover, when the compound has the general formula I-1D, X is O or S;

when the compounds have the general formulas I-1A and I-1D,

R1is selected from hydrogen, halogen, cyano, nitro, amino, carboxyl, C1-C4alkyl, halogenated C1-C4alkyl, C3-C4cycloalkyl, C1-C4alkoxyl, halogenated C1-C4alkoxyl, C1-C4alkylthio, halogenated C1-C4alkylthio, C1-C4alkylsulfinyl, C1-C4alkylsulfonyl, C2-C4alkenyl, halogenated C2-C4alkenyl, C2-C4alkynyl, halogenated C2-C4alkynyl, C3-C4alkenyloxy, halogenated C3-C4alkenyloxy, C1-C4alkynyloxy, halogenated C3-C4alkynyloxy, C1-C4alkylamino, di(C1-C4alkyl) amino, C1-C4alkylaminocarbonyl, halogenated C1-C4alkylaminocarbonyl, C1-C4alkoxycarbonyl, halogenated C1-C4alkoxycarbonyl, C1-C4alkoxy C1-C4alkyl or C1-C4alkylthio C1-C4alkyl;

R2is selected from hydrogen, halogen, cyano, nitro, amino, carboxyl, formyl, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxy or halogenated C1-C4alkoxy;

when the compounds have the general formulas I-1A, I-1B and I-1C,

R3is selected from hydrogen, hydroxyl, formyl, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxy, halogenated C1-C4alkoxy, C3-C4cycloalkyl, C1-C4alkylthio, C2-C4alkenylthio, C2-C4alkenyl, C2-C4alkynyl, halogenated C2-C4alkenyl, halogenated C2-C4alkynyl, C1-C4alkoxy C1-C4alkyl, halogenated C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, halogenated C1-C4alkylthio C1-C4alkyl, C1-C4alkylsulfinyl, halogenated C1-C4alkylsulfinyl, C1-C4alkylsulfonyl, halogenated C1-C4alkylsulfonyl, C1-C4alkylaminosulfonyl, di(C1-C4alkyl) aminosulfonyl, C1-C4alkylsulfonylaminocarbonyl, C1-C4alkylcarbonylaminosulfonyl, C3-C4cycloalkyloxycarbonyl, C1-C4alkylcarbonyl, halogenated C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, halogenated C1-C4alkoxycarbonyl, C1-C4alkylcarbonyl C1-C4alkyl, C1-C4alkoxycarbonyl C1-C4alkyl, C1-C4alkylaminocarbonyl, di(C1-C4alkyl) aminocarbonyl, C2-C4alkenyloxycarbonyl, C2-C4alkynyloxycarbonyl, C1-C4alkoxy C1-C4alkoxycarbonyl, C1-C4alkylaminothio, di(C1-C4alkyl) aminothio, and unsubstituted or substituted arylcarbonyl C1-C4alkyl, arylcarbonyl, aryloxycarbonyl, aryl C1-C4alkyloxycarbonyl, aryl C1-C4alkyl, heteroarylcarbonyl C1-C4alkyl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroaryl C1-C4alkyloxycarbonyl and heteroaryl C1-C4alkyl by 1-5 of the following groups; the following groups are halogen, nitro, cyano, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxy or halogenated C1-C4alkoxy;

when the compound has the general formula I-1B,

R13, R14, R15and R16are the same or different and are respectively selected from hydrogen, halogen, hydroxyl, amino, cyano, nitro, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxy, halogenated C1-C4alkoxy or C3-C4cycloalkyl;

when the compound has the general formula I-1C,

R17and R18are the same or different and are selected from hydrogen, halogen, C1-C4alkyl, halogenated C1-C4alkyl, C1-C4alkoxyl, halogenated C1-C4alkoxyl, C1-C4alkylthio, halogenated C1-C4alkylthio, C3-C4cycloalkyl, and unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

or salt formed by the compounds shown by general formulas I-1A, I-1B, I-1C and I-1D and hydrochloric acid, sulfuric acid, phosphoric acid, formic acid, acetic acid, trifluoroacetic acid, oxalic acid, methanesulfonic acid, p-toluenesulfonic acid, benzoic acid, phthalic acid, maleic acid, fumaric acid, sorbic acid, malic acid or citric acid.

In the pyrimidine-containing substituted pyrazole compound of the present invention, a more further optional compound comprises: in the compounds shown by the general formulas I-1A, I-1B, I-1C and I-1D:

R4and R5are the same or different and are selected from hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, methoxyl, ethoxyl, n-propoxy, isopropoxy, n-butoxy, sec-butoxy, isobutoxy or tert-butoxy;

R6and R7are the same or different and are respectively selected from hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, methoxyl, ethoxyl, n-propoxy, isopropoxy, n-butoxy, sec-butoxy, isobutoxy or tert-butoxy;

R8and R9are the same or different and are respectively selected from hydrogen, cyano, fluorine, chlorine, bromine, iodine, methyl, ethyl or trifluoromethyl;

R10is selected from fluorine, chlorine, bromine, iodine, cyano, amino, nitro, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, trifluoromethyl, trichloromethyl, difluoromonochloromethyl, dichloromonofluoromethyl, methoxyl, ethoxyl, n-propoxy, isopropoxy, n-butoxy, sec-butoxy, isobutoxy, t-butoxy, methylthio, ethylthio, trifluoromethoxy, trifluoroethoxy, methoxycarbonyl, ethoxycarbonyl, aminocarbonyl, methylaminocarbonyl, ethylaminocarbonyl or dimethylaminocarbonyl;

n is selected from an integer from 0 to 5; when n is 0, a benzene ring has no substituent; when n is greater than 1, R10may be the same or different;

W is selected from hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, t-butyl, monofluoromethyl, monochloromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl, methoxyl, ethoxyl, methylthio, ethylthio, methylsulfonyl or ethylsulfonyl;

moreover, when the compound has the general formula I-1D, X is O or S;

when the compounds have the general formulas I-1A and I-1D,

R1is selected from hydrogen, fluorine, chlorine, bromine, iodine, cyano, nitro, amino, carboxyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, monofluoromethyl, monochloromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl, methoxymethyl, ethoxymethyl or trifluoroethoxymethyl;

R2is selected from hydrogen, fluorine, chlorine, bromine, iodine, cyano, nitro, amino, carboxyl, formyl, methyl, ethyl, methoxy, ethoxy or trifluoroethoxy;

when the compounds have the general formulas I-1A, I-1B and I-1C,

R3is selected from hydrogen, hydroxyl, formyl, acetyl, propanoyl, butyryl, trifluoroacetyl, benzoyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, trifluoromethyl, trifluoroethyl, methoxyl, ethoxyl, trifluoroethoxy, cyclopropyloxy, methylthio, ethylthio, allyl, propargyl, mesyl, ethylsulfonyl, trifluoroethylsulfonyl, methylaminosulfonyl, ethylaminosulfonyl, dimethylaminosulfonyl, diethylaminosulfonyl, methylsulfonylaminocarbonyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, methylaminocarbonyl, dimethylaminocarbonyl, vinyloxycarbonyl, ethynyloxycarbonyl, methylaminothio, ethylaminothio or dimethylaminothio;

when the compound has the general formula I-1B,

R13, R14, R5and R16are the same or different and are respectively selected from hydrogen, fluorine, chlorine, bromine, iodine, amino, cyano, nitro, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, trifluoromethyl, trichloromethyl, difluoromonochloromethyl, dichloromonofluoromethyl, methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, sec-butoxy, isobutoxy, t-butoxy, trifluoromethoxy or trifluoroethoxy;

when the compound has the general formula I-1C,

R17and R18are the same or different and are respectively selected from hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, trifluoromethyl, trichloromethyl, difluoromonochloromethyl, dichloromonofluoromethyl, trifluoroethyl, methoxyl, ethoxyl, n-propoxy, isopropoxy, n-butoxy, sec-butoxy, isobutoxy, tert-butoxy, trifluoromethoxy, trifluoroethoxy, and unsubstituted or substituted aryl, arylmethyl, arylcarbonyl, arylmethylcarbonyl, aryloxycarbonyl, heteroaryl, heteroarylmethyl, heteroarylcarbonyl, heteroarylmethylcarbonyl or heteroaryloxycarbonyl by one to five R10;

or salt formed by the compounds shown by general formulas I-1A, I-1B, I-1C and I-1D and hydrochloric acid, sulfuric acid, phosphoric acid, formic acid, acetic acid, trifluoroacetic acid, oxalic acid, methanesulfonic acid, p-toluenesulfonic acid, benzoic acid, phthalic acid, maleic acid, fumaric acid, sorbic acid, malic acid or citric acid.

In the substituted pyrimidine compound of the present invention, a still further optional compound comprises: in the compounds shown by the general formulas I-1A, I-1B, I-1C and I-1D:

R4and R5are the same or different, and are respectively selected from hydrogen, fluorine, chlorine, bromine or methyl;

R6and R7are selected from hydrogen;

R8is hydrogen or methyl;

R9is selected from hydrogen or methyl;

R10is selected from fluorine, chlorine, bromine, iodine, cyano, nitro, methyl, ethyl, trifluoromethyl, methoxy, methylthio or trifluoromethoxy;

n is selected from an integer from 0 to 5; when n is 0, the benzene ring has no substituent; when n is greater than 1, R10can be the same or different;

W is selected from hydrogen, fluorine, chlorine, bromine, iodine or methyl;

moreover, when the compound has the general formula I-1D, X is O or S;

when the compounds have the general formulas I-1A and I-1D,

R1is selected from hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl or difluoromethyl;

R2is selected from hydrogen, fluorine, chlorine, bromine, iodine, nitro, amino, formyl, methyl, ethyl, methoxy or ethoxy;

when the compounds have the general formulas I-1A, I-1B and I-1C,

R3is selected from hydrogen, methyl, acetyl, trifluoroacetyl, methoxy, methylthio, allyl, methanesulfonyl, methylaminosulfonyl, dimethylaminosulfonyl, methoxycarbonyl, methylaminocarbonyl, dimethylaminocarbonyl, methylaminothio or dimethylaminothio;

when the compound has the general formula I-1B,

R13, R14, R15and R16are the same or different and are respectively selected from hydrogen, fluorine, chlorine, bromine, iodine or methyl;

when the compound has the general formula I-1C,

R17and R18are the same or different and are respectively selected from hydrogen, fluorine, chlorine, bromine or iodine;

or salt formed by the compounds shown by general formulas I-1A, I-1B, I-1C and I-1D and hydrochloric acid, sulfuric acid, phosphoric acid, formic acid, acetic acid, trifluoroacetic acid, oxalic acid, methanesulfonic acid, p-toluenesulfonic acid, benzoic acid, phthalic acid, maleic acid, fumaric acid, sorbic acid, malic acid or citric acid.

In the substituted pyrimidine compound of the present invention, a more optional compound comprises: in the compounds shown by the general formulas I-1A, I-1B, I-1C and I-1D:

R4and R5can be the same or different, and are respectively selected from hydrogen or methyl;

R6and R7are selected from hydrogen;

R8is hydrogen or methyl;

R9is selected from methyl;

R10is selected from fluorine, chlorine, bromine, iodine, cyano, nitro, methyl, ethyl, trifluoromethyl, methoxy, methylthio or trifluoromethoxy;

n is selected from an integer from 1 to 5; when n is greater than 1, R10can be the same or different;

W is selected from hydrogen, fluorine, chlorine, bromine or iodine;

moreover, when the compound has the general formula I-1D, X is O or S;

when the compounds have the general formulas I-1A and I-1D,

R1is selected from fluorine, chlorine, bromine, iodine, methyl, ethyl or difluoromethyl;

R2is selected from fluorine, chlorine, bromine, iodine, nitro, amino, formyl, methyl or methoxyl;

when the compounds have the general formulas I-1A, I-1B and I-1C,

R3is selected from hydrogen, methyl, acetyl, methoxyl, allyl, methanesulfonyl, methoxycarbonyl, methylaminocarbonyl, dimethylaminocarbonyl or dimethylaminothio;

when the compound has the general formula I-1B,

R13, R14, R15and R16are selected from hydrogen;

when the compound has the general formula I-1C,

R17is selected from hydrogen;

R18is selected from chlorine;

or salt formed by the compounds shown by general formulas I-1A, I-1B, I-1C and I-1D and hydrochloric acid, sulfuric acid, phosphoric acid, formic acid, acetic acid, trifluoroacetic acid, oxalic acid, methanesulfonic acid, p-toluenesulfonic acid, benzoic acid, phthalic acid, maleic acid, fumaric acid, sorbic acid, malic acid or citric acid.

A preparation method of the substituted pyrimidine compound is provided. The preparation method of the compound shown by the general formula I is:



A use of the substituted pyrimidine compound shown by the general formula I as a fungicide, insecticide and acaricide drug is provided. Further, a use of the compound as a fungicide, insecticide and acaricide drug in agriculture or other fields is provided.

A fungicidal, insecticidal and acaricidal composition is provided. The composition uses the substituted pyrimidine compound shown by the general formula I as an active ingredient, wherein the weight percentage of the active ingredient in the composition is 0.1-99%.

In the definitions of the compounds of the general formula I provided above, the terms used in the collection are generally defined as follows:

Halogen: fluorine, chlorine, bromine or iodine. Alkyl: linear or branched alkyl, such as methyl, ethyl, propyl, isopropyl, n-butyl or tert-butyl. Cycloalkyl: substituted or unsubstituted cyclic alkyl, such as cyclopropyl, cyclopentyl or cyclohexyl. Substituents, such as methyl and halogen. Haloalkyl: linear or branched alkyl on which hydrogen atoms can be partially or fully replaced by halogen atoms, such as chloromethyl, dichloromethyl, trichloromethyl, fluoromethyl, difluoromethyl and trifluoromethyl. Alkylsulfinyl: linear or branched alkyl, connected to the structure through sulfinyl (—SO—), such as methylsulfinyl. Halogenated alkylsulfinyl: linear or branched alkylsulfinyl, and hydrogen atoms on the alkyl can be partially or fully replaced by halogen atoms. Halogenated alkylsulfonyl: linear or branched alkylsulfonyl, and hydrogen atoms on the alkyl can be partially or fully replaced by halogen atoms. Alkylaminothio: such as CH3NHS— and C2H5NHS—. Dialkylaminothio: such as (CH3)2NS— and —(C2H5)2NS—. Alkylaminosulfonyl: alkyl-NH—SO2—. Dialkylaminosulfonyl: (alkyl)2-N—SO2—. Alkylsulfonylaminocarbonyl: alkyl-SO2—NH—CO—. Alkylcarbonylaminosulfonyl: alkyl-CO—NH—SO2—. Alkylcarbonylalkyl: alkyl-CO-alkyl-. Alkylsulfonyloxy: alkyl-S(O)2—. Halogenated alkylsulfonyloxy: hydrogen atoms on alkyl of alkylsulfonyloxy can be partially or fully replaced by halogen atoms, such as CF3-SO2—O. Cycloalkyloxycarbonyl: such as cyclopropoxycarbonyl, cyclohexyloxycarbonyl and the like. Alkoxy: linear or branched alkyl, bonded to the structure through an oxygen atom. Halogenated alkoxyl: linear or branched alkoxyl, and hydrogen atoms on the alkoxyl can be partially or fully replaced by halogen atoms. For example, chloromethoxy, dichoromethoxy, trichloromethoxy, fluoromethoxy, difluoromethoxy, trifluoromethoxy, chlorofluoromethoxy, trifluoroethoxy and the like. Halogenated alkoxycarbonyl: hydrogen atoms on alkyl of alkoxycarbonyl can be partially or fully replaced by halogen atoms, such as ClCH2CH2OCO—, CF3CH2OCO— and the like. Alkoxyalkyl: alkyl-O-alkyl-, such as CH3OCH2—. Halogenated alkoxyalkyl: hydrogen atoms on alkyl of alkoxyalkyl can be partially or fully replaced by halogen atoms, such as CCH2CH2OCH2—, CF3CH2OCH2— and the like. Alkoxycarbonyl-alkyl: alkoxycarbonyl-alkyl-, such as CH3OCOCH2—. Halogenated alkoxycarbonylalkyl: hydrogen atoms on alkyl of alkoxycarbonylalkyl can be partially or fully replaced by halogen atoms, such as CF3CH2OCOCH2—. Alkylcarbonyloxy: such as CH3COO—, and the like. Halogenated alkylcarbonyloxy: hydrogen of alkylcarbonyloxy can be partially or fully replaced by halogen atoms, such as CF3COO—, and the like. Alkoxycarbonyloxy: alkoxycarbonyl-oxy-, such as CH3OCOO—. Halogenated alkoxycarbonyloxy: hydrogen atoms on alkyl of alkoxycarbonyloxy can be partially or fully replaced by halogen atoms, such as CF30COO—. Alkylthiocarbonylalkyl: alkylthiocarbonyl-alkyl-, such as CH3SCOCH2—, halogenated alkylthiocarbonylalkyl: hydrogen atoms on alkyl of alkylthiocarbonylalkyl can be partially or fully replaced by halogen atoms, such as CF3CH2SCOCH2—. Alkoxyalkoxy: such as CH3OCH2O—, and the like. Halogenated alkoxyalkoxy: hydrogen atoms on alkoxyalkoxy can be partially or fully replaced by halogen atoms, such as CF3OCH2O—. Alkoxyalkoxycarbonyl: such as CH3OCH2CH2CO—, and the like. Alkylthio: linear or branched alkyl, bonded to the structure through a sulfur atom. Halogenated alkylthio: linear or branched alkylthio, and hydrogen atoms on the alkyls can be partially or fully replaced by halogen atoms. For example, chloromethylthio, dichloromethylthio, trichloromethylthio, fluoromethylthio, difluoromethylthio, trifluoromethylthio, chlorofluoromethylthio, and the like. Alkylthioalkyl: alkyl-S-alkyl-, such as CH3SCH2—. Halogenated alkylthioalkyl: hydrogen atoms on alkyl of alkylthioalkyl can be partially or fully replaced by halogen atoms, such as ClCH2CH2SCH2—, CF3CH2SCH2—, and the like. Alkylamino: linear or branched alkyl, bonded to the structure through a nitrogen atom. Halogenated alkylamino: linear or branched alkylamino, and hydrogen atoms on the alkyl can be partially or fully replaced by halogen atoms. Dialkylamino: such as (CH3)2N— and (CH3CH2)2N—. Halogenated dialkylamino: hydrogen atoms on alkyl can be partially or fully replaced by halogen atoms, such as (CF3)2N— and (CF3CH2)2N—. Alkenyl: linear or branched alkene, such as vinyl, 1-propenyl, 2-propenyl and different butenyl, pentenyl and hexenyl isomers. The alkenyl also comprises polyenes, such as 1,2-propadienyl and 2,4-hexadienyl. Halogenated alkenyl: linear or branched alkene, and hydrogen atoms on the alkenyl can be partially or fully replaced by halogen atoms. Alkenyloxy: linear or branched alkene, bonded to the structure through an oxygen atom. Halogenated alkenyloxy: linear or branched alkenyloxy, and hydrogen atoms on the alkenyloxy can be partially or fully replaced by halogen atoms. Alkenylthio: linear or branched alkene, bonded to the structure through a sulphur atom. For example, CH2═CHCH2S—. Alkenoxycarbonyl: such as CH2═CHCH2OCO—, and the like. Alkynyl: linear or branched alkyne, such as ethynyl, 1-propynyl, 2-propynyl and different butynyl, pentynyl and hexynyl isomers. The alkynyl also comprises a group consisting of multiple triple bonds, such as 2,5-hexadiynyl. Halogenated alkynyl: linear or branched alkyne, and hydrogen atoms on the alkynyl can be partially or fully replaced by halogen atoms. Alkynyloxy: linear or branched alkyne, bonded to the structure through an oxygen atom. Halogenated alkynyloxy: linear or branched alkynyloxy, and hydrogen atoms on the alkynyloxy can be partially or fully replaced by halogen atoms. Alkynyloxycarbonyl, such as CH═CCH2OCO—, and the like. Alkylsulfonyl: linear or branched alkyl, connected to the structure through sulfonyl (—SO2—), such as methylsulfonyl. Halogenated alkylsulfonyl: linear or branched alkylsulfonyl, and hydrogen atoms on the alkyl can be partially or fully replaced by halogen atoms. Alkylcarbonyl: alkyl, connected to the structure through carbonyl, such as CH3CO— and CH3CH2CO—. Halogenated alkylcarbonyl: hydrogen atoms on alkyl of alkylcarbonyl can be partially or fully replaced by halogen atoms, such as CF3CO—. Alkoxycarbonyl: alkoxyl, connected to the structure through carbonyl, such as CH3OCO— and CH3CH2CO—. Aminocarbonyl: such as NH2CO—. Alkylaminocarbonyl: alkyl-NH—CO—, such as CH3NHCO— and CH3CH2NHCO—. Dialkylaminocarbonyl: such as (CH3)2NCO— and (CH3CH2)2NCO—. Aryl parts of (hetero) aryl, (hetero) arylalkyl, (hetero) arylcarbonyl, (hetero) arylmethylcarbonyl, (hetero) arylcarbonylalkyl, (hetero) aryloxycarbonyl and (hetero) arylalkyloxycarbonyl comprise phenyl or naphthyl. Heteroaryl is a five-membered or six-membered ring containing one or more N, O and S hetero atoms, such as furyl, pyrazolyl, thiazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, quinolinyl, and the like. (Hetero) aryl: such as phenyl, and the like. (Hetero) arylalkyl: such as benzyl, phenethyl, parachloro-benzyl, 2-chloropyridine-5-yl, 2-chloro-thiazol-5-yl, and the like. (Hetero) arylcarbonyl: such as benzoyl, 4-chlorobenzoyl, and the like. (Hetero) arylmethylcarbonyl: such as PhCH2CO—. (Hetero) arylcarbonylalkyl: such as PhCOCH2—. (Hetero) aryloxycarbonyl: such as phenoxycarbonyl, 4-chlorophenoxycarbonyl, 4-nitrophenoxycarbonyl, naphthyloxycarbonyl, and the like. Arylalkyloxycarbonyl: such as benzyloxycarbonyl, 4-chlorobenzyloxycarbonyl, 4-trifluoromethylbenzyloxycarbonyl, and the like. (Hetero) arylalkyloxycarbonyl: such as PhCH2OCO—, 4-Cl-PhCH2OCO—, and the like.

Table 1, Table 2, Table 3, Table 4, Table 5, Table 6, Table 7 and Table 8 respectively list some specific substituents of R1, R2, R3(X═NR3), R4, R5, R6, R7, R8, R9and W in the general formula I, but not limited to the substituents.



TABLE 1R1SubstituentsR1HIi-C3H7i-C4H9CH2ClCH(CH3)ClC≡CHCNCOOCH3OCH3OCH2CH═CHClCONH2NHC2H5CH2OCH2CH3CH2CH2CH2OCH2CH3FCH3n-C4H9CF3CHBr2CH(CH3)BrSCH3NO2COOC2H5OC2H5OCH2C≡CHCONHCH2N(CH3)2CH2CH2OCH3ClC2H5s-C4H9CCl3CF3CH2C(CH3)2FSOCH3NH2CH3NHOCF3OCH2C≡C-1CON(CH3)2N(C2H5)2CH2CH2OCH2CH3Brn-C3H7i-C4H9CHF2CH(CH3)FCH═CH2SO2CH3COOHC2H5NHOCH2CH═CH2OCH2C≡CCH3NHCH3CH2OCH3CH2CH2CH2OCH3

TABLE 2R2SubstituentR2R2R2R2HFClBrICNNO2NH2CHOCH3C2H5n-C3H7i-C3H7n-C4H9s-C4H9i-C4H9t-C4H9OCH3OC2H5OC3H7-nOC3H7-iOC4H9-nOC4H9-iOC4H9-iOCH2FOCHF2OCF3OCH2CF3

TABLE 3R3SubstituentR3HCH3n-C4H9CH2BrCH2ClOCH3OCF3SCH3CH2CH═CH2CH2C≡C-1CH2CH2OCH2CH3CH2SCH3CH2SCH2ClSOC2H5SO2C2H5SO2NHCH3COC2H5CO-i-C4H9COOCH3COOCF3CH2COOC2H5CONHC2H5COOCH2CH═CH2SNHCH3OHC2H5i-C4H9CHF2CHCl2OC2H5OCH2CF3SC2H5CH2CH═CCl2CH2OCH3CH2OCH2ClCH2SCH2CH3CH2SCH2CH2ClSOCF3SO2CF3SO2N(CH3)3CO-n-C3H7CO-t-C4H9COOC2H5COOCH2CH2ClCH2COCH3CONH-t-C4H9COOCH2C≡CHSNHC2H5—C(═O)Hn-C3H7i-C4H9CHBr2CCl2OCH(CH3)2OCH2FSCH2CH═CH2C≡CHCH2OCH2CH3CH2OCH2CH2ClCH2CH2SCH3CH2CH2SCH2ClSOCH2CF3SO2CH2CF3CONHSCO2CH3CO-i-C3H7COCF3COO-n-C3H7COOCH2CF3CH2COC2H5CON(CH3)2COOCH2OCH3SN(CH3)2CBr3i-C3H7CCl3CF3CH2FOC(CH3)3OCHF3CH═CH3CH2C≡CHCH2CH2OCH3CH2CH2OCH2ClCH2CH2SCH2CH3SOCH3SO2CH3SO2NHCOCH3COCH5CO-n-C4H9COCH2ClCOO-t-C4H9CH2COOCH3CONHCH3CON(C2H5)2COOCH2CH2OCH3SN(C2H5)2

TABLE 4R4(R5) SubstituentR4(R5)R4(R5)R4(R5)R4(R5)HFClBrICH3C2H5n-C3H7i-C3H7n-C4H9s-C4H9i-C4H9t-C4H9CF3CCl3CHF2CH2ClCHBr2CF3CH2CH(CH3)FCH(CH3)ClCH(CH3)BrC(CH3)2FOCH3OC2H5n-C3H7Oi-C3H7On-C4H9Os-C4H9Oi-C4H9Ot-C4H9OOCF3OCH2CF3CR4R5

TABLE 5R6(R7) SubstituentR6(R7)R6(R7)R6(R7)R6(R7)HFClBrICH3C2H5n-C3H7i-C3H7n-C4H9s-C4H9i-C4H9t-C4H9CF3CCl3CHF2CH2ClCHBr2CF3CH2CH(CH3)FCH(CH3)ClCH(CH3)BrC(CH3)2FOCH3OC2H5n-C3H7Oi-C3H7On-C4H9Os-C4H9Oi-C4H9Ot-C4H9OOCF3OCH2CF3CR6R7

TABLE 6R8SubstituentR8R8R8R8HCNCH3C2H5n-C3H7i-C3H7n-C4H9s-C4H9i-C4H9i-C4H9CF3CCl3CHF2CH2FCH2ClCH2CF3CF2CF3COOCH3PhPh-4-Cl

TABLE 7R9SubstituentR10R10R10R10R10CH3Etn-Pri-Prn-Bui-Bus-But-BuCH2FCHF2CF3CH2CF3COCH3COEtCO-n-PrCO-n-BuCO-t-BuCOCF3CO2CH3CO2EtCO2-n-PrCO2-i-PrCO2-t-BuCO2CH2CF3CH2OCH3

TABLE 8W SubstituentWWWWWHi-C3H7CHF2OCH3SCH3Fn-C4H9CHBr2OC2H5SC2H5Cli-C4H9CF3OC3H7-nSC3H7-nBrCH3CH(CH3)FOC3H7-iSC3H7-iIC2H5CH(CH3)ClOC4H9-iSC4H9-nCHCl2CCl3CH(CH3)Br CH(n-C4H9)FOC4H9-i OC4H9-tSC4H9-i SC4H9-tC(CH3)2F n-C3H7OCF3OCH2CF3SO2CH3t-C4H9

Part of compounds in the present invention can be illustrated by specific compounds listed in Table 9 to Table 32, but not to limit the present invention. In the general formula compounds I-1A, I-1B, I-1C and I-1D involved in the table, W═R6═R7═R13═R14═R15═R16═R17═H, R9═CH3.

In the general formula I-1A,



When R1═Cl, R2═Cl, R3═R4═R5═H, R8═H, m=1, the (R10)n substituent is shown in Table 9, and the numbers of representative compounds are successively 9-1 to 9-288.

TABLE 9No.(R10)n9-1H9-22-F9-33-F9-44-F9-52,3-diF9-62,4-diF9-72,5-diF9-82,6-diF9-93,4-diF9-103,5-diF9-112,3,4-triF9-122,3,5-triF9-132,4,5-triF9-142,3,6-triF9-152,4,6-triF9-163,4,5-triF9-172-Cl9-183-Cl9-194-Cl9-202,3-diCl9-212,4-diCl9-222,5-diCl9-232,6-diCl9-243,4-diCl9-253,5-diCl9-262,3,4-triCl9-272,3,5-triCl9-282,4,5-triCl9-292,3,6-triCl9-302,4,6-triCl9-313,4,5-triCl9-322-Br9-333-Br9-344-Br9-352,3-diBr9-362,4-diBr9-372,5-diBr9-382,6-diBr9-393,4-diBr9-403,5-diBr9-412,3,4-triBr9-422,3,5-triBr9-432,4,5-triBr9-442,3,6-triBr9-452,4,6-triBr9-463,4,5-triBr9-472-CN9-483-CN9-494-CN9-502-NO29-513-NO29-524-NO29-532,4-diNO29-542,4,6-3NO29-552-CH39-563-CH39-574-CH39-582,3-diCH39-592,4-diCH39-602,5-diCH39-612,6-diCH39-623,4-diCH39-633,5-diCH39-642-C2H59-653-C2H59-664-C2H59-672-CF39-683-CF39-694-CF39-702-OCH39-713-OCH39-724-OCH39-732-SCH39-743-SCH39-754-SCH39-762-OCF39-773-OCF39-784-OCF39-792-SCF39-803-SCF39-814-SCF39-822-OC2H59-833-OC2H59-844-OC2H59-852-NHCH39-863-NHCH39-874-NHCH39-882-N(CH3)29-893-N(CH3)29-904-N(CH3)29-912-COCH39-923-COCH39-934-COCH39-942-COC2H59-953-COC2H59-964-COC2H59-972-SO2CH39-983-SO2CH39-994-SO2CH39-1002-OCHF29-1013-OCHF29-1024-OCHF29-1032-SO2C2H59-1043-SO2C2H59-1054-SO2C2H59-1062-CO2CH39-1073-CO2CH39-1084-CO2CH39-1092-CO2C2H59-1103-CO2C2H59-1114-CO2C2H59-1122-CH2OCH39-1133-CH2OCH39-1144-CH2OCH39-1152-OCOCH39-1163-OCOCH39-1174-OCOCH39-1182-OCOCH2CH39-1193-OCOCH2CH39-1204-OCOCH2CH39-1212-OCO2CH39-1223-OCO2CH39-1234-OCO2CH39-1242-OCH2OCH39-1253-OCH2OCH39-1264-OCH2OCH39-1272-OCF2OCF39-1283-OCF2OCF39-1294-OCF2OCF39-1302-COPh9-1313-COPh9-1324-COPh9-1332-COCH2Ph9-1343-COCH2Ph9-1354-COCH2Ph9-1362-NHPh9-1373-NHPh9-1384-NHPh9-1392-OPh9-1403-OPh9-1414-OPh9-1422-CONHPh9-1433-CONHPh9-1444-CONHPh9-1452-CO2Ph9-1463-CO2Ph9-1474-CO2Ph9-1482-CONH29-1493-CONH29-1504-CONH29-1512-Cl-4-F9-1522-Cl-4-Br9-1532-Cl-4-CH39-1542-Cl-4-CF39-1552-Cl-4-NO29-1562-Cl-4-CN9-1572-Cl-4-OCF39-1582-F-4-Cl9-1592-Br-4-Cl9-1602-CH3-4-Cl9-1612-CF3-4-Cl9-1622-NO2-4-Cl9-1632-CN-4-Cl9-1642-OCF3-4-Cl9-1652,6-diCl-4-NO29-1662,6-diCl-4-CF39-1672,6-diCl-4-CN9-1682,6-diCl-4-COCH39-1692,6-diCl-4-CONH29-1702,4-diCl-6-NO29-1712,4-diCl-6-CN9-1722,4-diCl-6-CF39-1732,4-diF-6-NO29-1742,6-diF-4-NO29-1752-NO2-4-F9-1762-NO2-4-Br9-1772-NO2-4-CF39-1782-NO2-4-CN9-1792-NO2-4-COCH39-1802-NO2-4-CONH29-1812-NO2-4-CH39-1822-NO2-4-OCH39-1832-NO2-4-SCH39-1842-NO2-4-NHCH39-1852-F-4-NO29-1862-Br-4-NO29-1872-CF3-4-NO29-1882-CN-4-NO29-1892-COCH3-4-NO29-1902-CONH2-4-NO29-1912-CH3-4-NO29-1922-Cl-4-F-6-NO29-1932-Cl-4-Br-6-NO29-1942-Cl-4-CH3-6-NO29-1952-Cl-4-CF3-6-NO29-1962-Cl-4,6-diNO29-1972-Cl-4-CN-6-NO29-1982-Cl-4-OCF3-6-NO29-1992-F-4-Cl-6-NO29-2002-Br-4-Cl-6-NO29-2012-CH3-4-Cl-6-NO29-2022-CF3-4-Cl-6-NO29-2034-Cl-2,6-diNO29-2042-CF3-4-CN9-2052-CN-4-CF39-2064-CF3-2,6-diNO29-2074-CN-2,6-diNO29-2084-CH3-2,6-diNO29-2094-OCF3-2,6-diNO29-2104-OCH3-2,6-diNO29-2114-SCH3-2,6-diNO29-2124-NHCH3-2,6-diNO29-2134-F-2,6-diNO29-2142-CF3-4,6-diNO29-2152-CN-4,6-diNO29-2162-CH3-4,6-diNO29-2172-F-4,6-diNO29-2182-OCF3-4,6-diNO29-2192-CF3-4-Br9-2203-CF3-4-NO29-2212-CN-4-Cl-6-NO29-2222-OCF3-4-Cl-6-NO29-2233-CF3-4-CN9-2243-CN-4-CF39-2252-CF3-4-Br-6-NO29-2263-NO2-4-CF39-2272-NO2-4-CN-5-CF39-2282-NO2-4-CF3-5-CN9-2294-OCF3-2,6-diBr9-2302-CH3-4-Cl-5-CH2CO2C2H59-2312,4-diCl-3-CH39-2322,4-diCl-3-CH3-6-NO29-2332-Cl-3-CH39-2342-CH3-3-Cl9-2352-CH3-3-Cl-4,6-diNO29-2362-CH3-3-Cl-4-NO29-2372-CH3-3-Cl-6-NO29-2382-Cl-3-CH3-4,6-diNO29-2392-Cl-3-CH3-4-NO29-2402-Cl-3-CH3-6-NO29-2412-Br-4-NO2-6-CN9-2423-Cl-4-CF3-2,6-diNO29-2432-NO2-4,5-diCl9-2442-NO2-3,5-diCl9-2452,5-diCl-4-NO29-2462,5-diCl-6-NO29-2472,3-diCl-4-NO29-2482,3-diCl-6-NO29-2493,4-diCl-2,6-diNO29-2502,5-diCl-4,6-diNO29-2512,4,5-triCl-6-NO29-2522,3,4-triCl-5-NO29-2532,3,4-triCl-6-NO29-2542,3,5-triCl-4,6-diCN9-2552,5-diCl-4-OCF2OCF39-2562,6-diBr-4-NO29-2572-F-4-NO2-6-Cl9-2582-Cl-4-NO2-6-SCN9-2592-Br-4-NO2-6-Cl9-2602-Cl-4-NO2-6-OCH39-2612-Cl-4-NO2-6-SCH39-2622-Cl-4-NO2-6-NHCH39-2632-Cl-4-NO2-6-SO2CH39-2642-Cl-4-SO2CH39-2652,6-diCl-4-SO2CH39-2662,6-diCl-4-CH39-2672,6-diCl-4-CO2CH39-2682,6-diCl-4-CONHCH39-2692,6-diCl-4-CON(CH3)29-2702,6-diCl-4-CF(CF3)29-2712-Cl-4-CF(CF3)2-6-Br9-2722-F-4-CF(CF3)2-6-Br9-2732-F-4-CF(CF3)2-6-Cl9-2742,6-diF-4-CF(CF3)2-6-Cl9-2752,4,5-triCl-3,6-2CN9-2762,3,5-triF-4,6-diCN9-2772-SO2NH29-2783-SO2NH29-2794-SO2NH29-2802-i-C3H79-2813-i-C3H79-2824-i-C3H79-2832-n-C4H99-2843-n-C4H99-2854-n-C4H99-2862-t-C4H99-2873-t-C4H99-2884-t-C4H9

Table 9-1: in the general formula I-1A, when R1═Cl, R2═CH3, R3═R4═R5═H, R8═H and m=1, the substituent (R10)n is identical to that in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 9-1-1 to 9-1-288.

Table 9-2: in the general formula I-1A, when R1═Cl, R2═OCH3, R3═R4═R5═H, R8═H and m=1, the substituent (R10)n is identical to that in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 9-2-1 to 9-2-288.

Table 9-3: in the general formula I-1A, when R1═Cl, R2═CHO, R3═R4═R5═H, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 9-3-1 to 9-3-288.

Table 9-4: in the general formula I-1A, when R1═Cl, R2═Br, R3═R4═R5═H, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 9-4-1 to 9-4-288.

Table 10: in the general formula I-1A, when R1═CH3, R2═Cl, R3═R4═R5═H, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 10-1 to 10-288.

Table 10-1: in the general formula I-1A, when R1═CH3, R2═Cl, R3═R4═R5═H, R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 10-1-1 to 10-1-288.

Table 10-2: in the general formula I-1A, when R1═CH3, R2═Cl, R3═R4═R5═H, R8═H and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 10-2-1 to 10-2-288.

Table 10-3: in the general formula I-1A, when R1═CH3, R2═Cl, R3═R4═R5═H, R8═CH3and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 10-3-1 to 10-3-288.

Table 10-4: in the general formula I-1A, when R1═CH3, R2═Cl, R3═R4═H, R5═R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 10-4-1 to 10-4-288.

Table 11: in the general formula I-1A, when R1═C2H5, R2═Cl, R3═R4═R5═H, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 11-1 to 11-288.

Table-11-1: in the general formula I-1A, when R1═C2H5, R2═Cl, R3═R4═R5═H, R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 11-1-1 to 11-1-288.

Table 11-2: in the general formula I-1A, when R1═C2H5, R2═Cl, R3═R4═R5═H, R8═H and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 11-2-1 to 11-2-288.

Table 11-3: in the general formula I-1A, when R1═C2H5, R2═Cl, R3═R4═R5═H, R8═CH3and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 11-3-1 to 11-3-288.

Table 11-4: in the general formula I-1A, when R1═C2H5, R2═Cl, R3═R4═H, R5═R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 11-4-1 to 1-4-288.

Table 12: in the general formula I-1A, when R1═CHF2, R2═Cl, R3═R4═R5═H, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 12-1 to 12-288.

Table 12-1: in the general formula I-1A, when R1═CHF2, R2═Cl, R3═R4═R5═H, R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 12-1-1 to 12-1-288.

Table 12-2: in the general formula I-1A, when R1═CHF2, R2═Cl, R3═R4═R5═H, R8═H and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9- to 9-288 of Table 9, and the numbers of representative compounds are successively 12-2-1 to 12-2-288.

Table 12-3: in the general formula I-1A, when R1═CHF2, R2═Cl, R3═R4═R5═H, R8═CH3and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 12-3-1 to 12-3-288.

Table 12-4: in the general formula I-1A, when R1═CHF2, R2═Cl, R3═R4═H, R5═R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 12-4-1 to 12-4-288.

Table 13: in the general formula I-1A, when R1═CF3, R2═Cl, R3═R4═R5═H, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 13-1 to 13-288.

Table 14: in the general formula I-1A, when R1═Cl, R2═Cl, R3═R4═H, R5═CH3, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 14-1 to 14-288.

Table 15: in the general formula I-1A, when R1═CH3, R2═Cl, R3═R4═H, R5═CH3, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 15-1 to 15-288.

Table 16: in the general formula I-1A, when R1═C2H5, R2═Cl, R3═R4═H, R5═CH3, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 16-1 to 16-288.

Table 17: in the general formula I-1A, when R1═CHF2, R2═Cl, R3═R4═H, R5═CH3, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 17-1 to 17-288.

Table 18: in the general formula I-1A, when R1═CF3, R2═Cl, R3═R4═H, R5═CH3, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 18-1 to 18-288.

In the general formula I-1B,



Table 19: in the general formula I-1B, when R3═R4═R5═H, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 19-1 to 19-288.

Table 19-1: in the general formula I-1B, when R3═R4═R5═H, R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 19-1-1 to 19-1-288.

Table 19-2: in the general formula I-1B, when R3═R4═R5═H, R8═H and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 19-2-1 to 19-2-288.

Table 19-3: in the general formula I-1B, when R3═R4═R5═H, R8═CH3and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 19-3-1 to 19-3-288.

Table 19-4: in the general formula I-1B, when R3═R4═H, R5═R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 19-4-1 to 19-4-288.

Table 20: in the general formula I-1B, when R3═R4═H, R5═CH3, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 20-1 to 20-288.

In the general formula I-1C,



Table 21: in the general formula I-1C, when R3═R4═R5═H, R18═Cl, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 21-1 to 21-288.

Table 21-1: in the general formula I-1C, when R3═R4═R5═H, R18═Cl, R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 21-1-1 to 21-1-288.

Table 21-2: in the general formula I-1C, when R3═R4═R5═H, R18═Cl, R8═H and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 21-2-1 to 21-2-288.

Table 21-3: in the general formula I-1C, when R3═R4═R5═H, R18═Cl, R8═CH3and m=2, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 21-3-1 to 21-3-288.

Table 21-4: in the general formula I-1C, when R3═R4═H, R18═Cl, R5═R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 21-4-1 to 21-4-288.

Table 22: in the general formula I-1C, when R3═R4═R5═H, R10═CH3, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 22-1 to 22-288.

Table 23: in the general formula I-1C, when R3═R4═H, R5═CH3, R18═Cl, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 23-1 to 23-288.

Table 24: in the general formula I-1C, when R3═R4═H, R5═CH3, R18═CH3, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 24-1 to 24-288.

In the general formula I-1D,



Table 25: in the general formula I-1D, when R1═CH3, R2═Cl, W=R4═R5H, X═O, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 25-1 to 25-288.

Table 26: in the general formula I-1D, when R1═C2H5, R2═Cl, W═R4═R5═H, X═O, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 26-1 to 26-288.

Table 26-1: in the general formula I-1D, when R1═C2H5, R2═Cl, W═R4═R5═H, X═O, R8═CH3and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 26-1-1 to 26-1-288.

Table 27: in the general formula I-1D, when R1═CHF2, R2═Cl, W═R4═R5═H, X═O, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 27-1 to 27-288.

Table 28: in the general formula I-1D, when R1═CH3, R2═Cl, W═R4═R5═H, X═S, R8═H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 28-1 to 28-288.

Table 29: in the general formula I-1D, when R1═C2H5, R2═Cl, W═R4═R5═H, X═S, R8=Hl and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 29-1 to 29-288.

Table 30: in the general formula I-1D, when R1═CHF2, R2═Cl, W═R4═R5═H, X═S, R$=H and m=1, the substituent (R10)n is identical to the substituent shown in Table 9, and sequentially corresponds to 9-1 to 9-288 of Table 9, and the numbers of representative compounds are successively 30-1 to 30-288.

In the general formula I-1A, when R1═CH3, R2═Cl, R4═R5═H, (R10)n=4-CH3, R8═H and m=1, the substituent R3(not hydrogen) is a different substituent as shown in Table 31, and the numbers of representative compounds are successively 31-1 to 31-140.

TABLE 31No.R3No.R3No.R3NoR331-1S-i-C3H731-2OH31-3—C(═O)H116-4CBr331-5CH331-6C2H531-7n-C3H7116-8i-C3H731-9n-C4H931-10i-C4H931-11i-C4H9116-12Cl331-13CH2Br31-14CHF231-15CHBr2116-16CF331-17CH2Cl31-18CHCl231-19CCl3116-20CH2F31-21OCH331-22OC2H531-23OCH(CH3)2116-24OC(CH3)331-25OCF331-26OCH2CF331-27OCH2F116-28OCHF231-29SCH331-30SC2H531-31SCH2CH═CH2116-32CH═CH231-33CH2CH═CH231-34CH2CH═CCl231-35C≡CH116-36CH2C≡CH31-37CH2C≡C-131-38CH2OCH331-39CH2OCH2CH3116-40CH2CH2OCH331-41CH2CH2OCH2CH331-42CH2OCH2Cl31-43CH2OCH2CH2Cl116-44CH2CH2OCH2Cl31-45CH2SCH331-46CH2SCH2CH331-47CH2CH2SCH3116-48CH2CH2SCH2CH331-49CH2SCH2Cl31-50CH2SCH2CH2Cl31-51CH2CH2SCH2Cl116-52SOCH331-53SOC2H531-54SOCF331-55SOCH2CF3116-56SO2CH331-57SO2C2H531-58SO2CF331-59SO2CH2CF3116-60SO2NHCOCH331-61SO2NHCH331-62SO2N(CH3)331-63CONHSO2CH3116-64COCH331-65COC2H531-66CO-n-C3H731-67CO-i-C3H7116-68CO-n-C4H931-69CO-i-C4H931-70CO-t-C4H931-71COCF3116-72COCH2Cl31-73COOCH331-74COOC2H531-75COO-N-C3H7116-76COO-t-C4H931-77COOCF331-78COOCH2CH2Cl31-79COOCH2CF3116-80CH2COOCH331-81CH2COOC2H531-82CH2COCH331-83CH2COC2H5116-84CONHCH331-85CONHC2H531-86CONH-t-C4H931-87CON(CH3)2116-88CON(C2H5)231-89COOCH2CH═CH231-90COOCH2C≡CH31-91COOCH2OCH3116-92COOCH2CH2OCH331-93SNHCH331-94SNHC2H531-95SN(CH3)2116-96SN(C2H5)231-9731-9831-99116-10031-10131-10231-10331-10431-10531-10631-10731-10831-10931-11031-11131-11231-11331-11431-11531-11631-11731-11831-11931-12031-12131-12231-12331-12431-12531-12631-12731-12831-12931-13031-13131-13231-13331-13431-13531-13631-13731-13831-13931-140

The salt of part of compounds in the present invention can be illustrated by the salt of specific compounds listed in Table 32, but not to limit the present invention.

TABLE 32Salt of Part of CompoundsNo.structure32-132-232-332-432-532-632-732-832-932-1032-1132-1232-1332-14

The compound of the present invention is prepared by the following method. Reaction formulas are as follows. Unless otherwise stated, the definitions of the groups in the formulas are the same as above:

The preparation method of the compound of the general formula I is as follows:



Intermediates 11 and 111 react in a suitable solvent under alkaline conditions to obtain the compound of the general formula I.

Proper alkali may be selected from, for example, potassium hydroxide, sodium hydroxide, sodium carbonate, potassium carbonate, sodium bicarbonate, triethylamine, pyridine, sodium methoxide, sodium ethoxide, sodium hydride, potassium tert-butoxide or sodium tert-butoxide.

The reaction is conducted in the proper solvent which can be selected from, for example, tetrahydrofuran, 1,4-dioxane, acetonitrile, toluene, xylene, benzene, N,N-dimethylformamide, N-methylpyrrolidone, dimethylsulfoxide, acetone or butanone.

The reaction temperature can be between room temperature and the boiling point temperature of the solvent, generally 20-100° C.

The reaction time is 30 minutes to 20 hours, generally 1-10 hours.

Intermediate 11 is commercially available and can also be prepared by known methods, for example, prepared by referring to the methods described in literature JP2000007662, U.S. Pat. Nos. 4,977,264, 6,090,815, US20040092402, JP09124613, U.S. Pat. Nos. 5,468,751, 4,985,426, 4,845,097, Journal of the American Chemical Society (1957), 79, 1455 Journal of Chemical Society (1955), p. 3478-3481.

Intermediate III is a key intermediate for the preparation of the compound of the general formula I in the present invention, and is prepared by the following method:



Intermediate M1 and dimethyl carbonate react in a suitable solvent at suitable temperature for 30 minutes to 20 hours, generally 1-10 hours, to obtain intermediate M2. Refer to Tetrahedron: Asymmetry, 24(15-16), 925-936; 2013 and Angewandte Chemie, International Edition, 53(45), 12210-12213; 2014 for the operation method of this step. M2 generates an electrophilic substitution reaction to obtain M3. Refer to Pest Management science, 66(1),2010,107-112 for the operation method of this step. M3 reacts with X1 to prepare M4. Refer to Pest Management science, 66(1),2010,107-112 for the operation method of this step. Finally, M4 reacts with the corresponding halogenide to prepare III. Refer to US20100158860, WO2011133444 and Bioorganic & Medicinal Chemistry, 20(20), 6109-6122, 2012 for the operation method of this step.

Further, the preparation method of the general formula compound I-1 is as follows: refer to corresponding steps and related reference literature of preparation of the compound of the general formula I for specific reaction conditions of the steps.



Intermediates II and III react in a suitable solvent under alkaline conditions to obtain the compound of the general formula I-1.

Proper alkali may be selected from, for example, potassium hydroxide, sodium hydroxide, sodium carbonate, potassium carbonate, sodium bicarbonate, triethylamine, pyridine, sodium methoxide, sodium ethoxide, sodium hydride, potassium tert-butoxide or sodium tert-butoxide.

The reaction is conducted in the proper solvent which can be selected from, for example, tetrahydrofuran, 1,4-dioxane, acetonitrile, toluene, xylene, benzene, N,N-dimethylformamide, N-methylpyrrolidone, dimethylsulfoxide, acetone or butanone.

The reaction temperature can be between room temperature and the boiling point temperature of the solvent, generally 20-100° C.

The reaction time is 30 minutes to 20 hours, generally 1-10 hours.

Intermediate II is commercially available and can also be prepared by known methods, for example, prepared by referring to the methods described in literature JP2000007662. U.S. Pat. Nos. 4,977,264, 6,090,815, US20040092402, JP09124613, U.S. Pat. Nos. 5,468,751, 4,985,426, 4,845,097, Journal of the American Chemical Society (1957), 79, 1455 Journal of Chemical Society (1955), p. 3478-3481.

Intermediate III is a key intermediate for the preparation of the compound of the general formula I-1 in the present invention, and is prepared by the following method:



Intermediate M1 and dimethyl carbonate react in a suitable solvent at suitable temperature for 30 minutes to 20 hours, generally 1-10 hours, to obtain intermediate M2. Refer to Tetrahedron: Asymmetry, 24(15-16), 925-936; 2013 and Angewandte Chemie, International Edition, 53(45), 12210-12213; 2014 for the operation method of this step. M2 generates an electrophilic substitution reaction to obtain M3. Refer to Pest Management science, 66(1),2010,107-112 for the operation method of this step. M3 reacts with X1 to prepare M4. Refer to CN102584705A for the operation method of this step. Finally, M4 reacts with the corresponding halogenide to prepare III. Refer to US20100158860, WO201133444 and Bioorganic & Medicinal Chemistry, 20(20), 6109-6122, 2012 for the operation method of this step.

Although the compound of the general formula I of the present invention and some compounds disclosed in the prior art also belong to pyrimidine-containing substituted pyrazole compounds, the structural features are still obviously different. Moreover, due to the structural differences, the compound of the present invention has better fungicidal, insecticidal and acaricidal activity.

The compound of the general formula I shows excellent activity against various fungi in agriculture or other fields, and also shows good activity against pests and mites. Therefore, the technical solution of the present invention also comprises the use of the compound of the general formula I as a fungicide, an insecticide and an acaricide in agriculture or other fields.

The examples of the diseases mentioned below are only used to explain the present invention, but not to limit the present invention.

The compound of the general formula I can be used for controlling the following diseases: oomycete diseases such as downy mildew (cucumber downy mildew, canola downy mildew, soybean downy mildew, beet downy mildew, sugar cane downy mildew, tobacco downy mildew, pea downy mildew, loofah downy mildew, winter melon downy mildew, melon downy mildew, cabbage downy mildew, spinach downy mildew, radish downy mildew, grape downy mildew and onion downy mildew), albugo candida (oilseed rape white rust and cabbage white rust), damping-off (oilseed rape damping-off, tobacco damping-off, tomato damping-off, pepper damping-off, eggplant damping-off, cucumber damping-off and cotton damping-off), pythium rot (chilli pythium rot, loofah pythium rot and winter melon pythium rot), blight (broad bean blight, cucumber blight, pumpkin blight, winter melon blight, watermelon blight, melon blight, pepper blight, leek blight, garlic blight and cotton blight), late blight (potato late blight and tomato late blight); fungi imperfecti diseases such as fusarium wilt (sweet potato wilt, cotton wilt, sesame wilt, castor wilt, tomato wilt, bean wilt, cucumber wilt, loofah wilt, pumpkin wilt, winter melon wilt, watermelon wilt, melon wilt, pepper wilt, broad bean wilt, rape wilt and soybean wilt), root rot (pepper root rot, eggplant root rot, bean root rot, cucumber root rot, bitter gourd root rot, cotton black root rot and broad bean root rot), wilt disease (cotton wilt disease, sesame wilt disease, pepper wilt disease, cucumber wilt disease and cabbage wilt disease), anthrax (sorghum anthrax, cotton anthrax, kenaf anthrax, jute anthrax, flax anthrax, tobacco anthrax, mulberry anthrax, pepper anthrax eggplant anthrax, bean anthrax, cucumber anthrax, bitter gourd anthrax, zucchini anthrax, winter melon anthrax, watermelon anthrax, melon anthrax and litchi anthrax), greensickness (cotton greensickness, sunflower greensickness, tomato greensickness, pepper greensickness and eggplant greensickness), scab (squash scab, winter melon scab and melon scab),Botrytis cinerea(cotton bollBotrytis cinerea, kennelBotrytis cinerea, tomatoBotrytis cinerea, pepperBotrytis cinerea, beanBotrytis cinerea, celeryBotrytis cinerea, spinachBotrytis cinereaand kiwiBotrytis cinerea), brown spot (cotton brown spot, jute brown spot, beet brown spot, peanut brown spot, pepper brown spot, winter melon brown spot, soybean brown spot, sunflower brown spot, pea brown spot and broad bean brown spot), black spot (flax false black spot, canola black spot, sesame black spot, sunflower black spot, castor black spot, tomato black spot, pepper black spot, eggplant black spot, bean black spot, cucumber black spot, celery black spot, carrot black rot, carrot black spot, apple black spot and peanut black spot), spot blight (tomato spot blight, pepper spot blight and celery spot blight), early blight (tomato early blight, pepper early blight, eggplant early blight, potato early blight and celery early blight), ring spot (soybean ring spot, sesame ring spot and bean ring spot), leaf blight (sesame leaf blight, sunflower leaf blight, watermelon leaf blight and melon leaf blight), stem rot (tomato stem rot and bean stem rot), and others (maize round spot, kenaf dropping disease, rice blast disease, foxtail millet black sheath, sugarcane eye spot, cotton boll aspergillosis, peanut crown rot, soybean stem blight, soybean black spot, melon leaf spot, peanut net blotch, tea red leaf spot,capsicumblight, winter melon leaf spot, celery black rot, spinach heart rot, kenaf leaf mold, kenaf spot, jute stem spot, soybean purple spot, sesame leaf spot,ricinusgray leaf spot, dark brown leaf spot, eggplantcercosporaleaf spot, bean southern blight, bitter gourd white spot, watermelon spot, jute blight rot, sunflower rhizome rot, bean char rot, soybean target spot, eggplant stick leaf spot, cucumber target spot, tomato leaf mold, eggplant leaf mold and broad bean chocolate spot); basidiomycete diseases such as rust (wheat stripe rust, wheat straw rust, wheat leaf rust, peanut rust, sunflower rust, sugar cane rust, leek rust, onion rust, chestnut rust and soybean rust), smut (maize head smut, corn smut, sorghum head smut, sorghum loose smut, sorghum covered kernel smut, sorghum stem smut, chestnut smut, sugar cane smut and bean rust) and others (such as wheat sheath blight and rice sheath blight disease, etc.); ascomycete diseases such as powdery mildew (wheat powdery mildew, rape powdery mildew, sesame powdery mildew, sunflower powdery mildew, sugar beet powdery mildew, eggplant powdery mildew, pea powdery mildew, loofah powdery mildew, pumpkin powdery mildew, zucchini powdery mildew, winter melon powdery mildew, melon powdery mildew, grape powdery mildew and broad bean powdery mildew),sclerotinia(flaxsclerotinia, rapesclerotinia, soybeansclerotinia, peanutsclerotinia, tobaccosclerotinia, capsicum sclerotinia, eggplantsclerotinia, beansclerotinia, peasclerotinia, cucumbersclerotinia, bitter gourdsclerotiorum, winter melonsclerotinia, watermelonsclerotiniaand celerysclerotinia), scab (apple scab and pear scab), etc.

The compound shown by the general formula I can be used for controlling the following pests and mites:

Coleoptera (beetle):acanthoscelidesspp. (curculionid),Acanthoscelides obtectus(commonBruchus pisorum),Agrilus planipennis, agriotesspp. (wireworm),Anoplophora glabripennis(Asian psacotheahilaris),anthonomusspp. (curculionidae),Anthonomus grandis(cotton bollworm),aphidiusspp.,apionspp. (curculionid),apogoniaspp. (grub),Atacnius spretulus(Maladera orientalis),Atomaria linearis(pygmy mangold beetle),aulacophorespp.,Bothynoderes punctiventris(beetroot weevil),bruchusspp. (curculionid),Bruchus pisorum(pea weevil),cacoesia(cacoesiaspp.),Callosobruchus maculatus(southern cowpea weevil),Carpophilus hemipteras(dried-frait beetle),Cassida vittata, cerosternaspp.,cerotoma(cecrotomaspp.) (chrysomcids),Cerotoma trifur cata(bean leaf beetle),ceutorhynchusspp. (curculionid),Ceutorhynchus assimilis(cabbage seedpod weevil),Ceutorhynchus napi(cabbagecurculio),chaetocnemaspp. (chrysomonad),colaspis(colaspisspp.) (soil beetle),Conoderus scalaris, Conoderus stigmosus, Conotrachelus nenuphar(plumcurculio),Cotinus nitidis(green June beetle),Crioceris asparagi(asparagus beetle),Cryptolestes ferrugincus(rusty grainbeetle),Cryptolestes pusillus(laemophloeidae),Cryptolestes turcicus(turkish grain beetle),ctenicera(cteniceraspp.) (nematode),curculiospp. (curculionid),cyclocephalaspp. (grub),Cylindroepturus adspersus(sunflower stem weevil),Deporaus marginatus(mango leaf-cutting weevil),Dermestes lardarius, Dermestes maculates, diabroticaspp. (leaf beetle),Epilachna varivcstis(Mexican bean beetle),Raustinus cubae, Hylobius pales(palesweevil),hyperaspp. (curculionid),Hypera postica, hyperdoes(hyperdoesspp.) (hyperodes weevil),Hypothenemus hampei(coffee fruit beetle),ipsspp. (engravers),Lasioderma serricome(cigarette beetle),Leptinotarsa decemlineata(Colorado potato beetle),Liogenys fuscus, Liogenys suturalis, Lissorhoptrus oryzophilus, lyctusspp. (powder post beetles),Maecolaspis joliveti, megascelis(megascelisspp.),Melanotus communis, meligethesspp.,Meligethes aeneus(blossom beetle),Melolontha melolontha(common European chafer),Oberea brevis, Oberea linearis, Oryctes rhinoceros(date palm beetle),Oryzaephilus mercator(merchant grain beetle),Oryzaephilus surinamensis(sawtoothed grain beetle),otiorhynchusspp. (curculionid),Oulema melanopus(cereal leafbeetle),Oulema oryzae, pantomorusspp. (curculionid),phyllophagaspp. (Melolontha melolontha/June scarabaeidae),Phyllophaga cuyabana, phyllotretaspp. (chrysomonad),phynchitesspp.,Popillia japonica(Japanese chafer),Prostephanus truncates(larger grain borer),Rhizopertha dominica(lesser grain borer),rhizotrogusspp. (Eurpoean chafer),rhynchophorusspp. (curculionid),scolytusspp. (wood moth),shenophorus(shenophorusspp.) (granary weevil),Sitona lincatus(pea leaf weevil),sitophilusspp. (valley weevil),Sitophilus granaries(granary weevil),Sitophilus oryzae(rice weevil),Stegobium paniceum(drugstore beetle),triboliumspp. (Tenebrio molitor),Tribolium castaneum(red flour beetle),Tribolium confusum(confused flour beetle),Trogoderma variabile(warehouse beetle) andZabrus tenebioides.

Dermaptera (earwig).

Dictyoptera (cockroach):Blattella germanica(German cockroach),Blatta orientalis)(oriental cockroach),Parcoblatta pennylvanica, Periplaneta americana(American cockroach),Periplaneta australoasiae(Australian cockroach),Periplancta brunnca(brown cockroach),Periplaneta fuliginosa(smokybrown cockroach),Pyncoselus suninamensis(surinam cockroach) andSupella longipalpa(brownbanded cockroach).

Diptera)(fly):aedesspp. (mosquito),Agromyza frontella(alfalfa blotch leafminer),agromyzaspp. (leaf miner),anastrephaspp. (fruit fly),Anastrepha suspensa(Caribbean fruit fly),anophelesspp. (mosquito),batroceraspp. (fruit fly),Bactrocera cucurbitae(melon fly),Bactrocera dorsalis(oriental fruit fly),ceratitisspp. (fruit fly),Ceratitis capitata(mediterranean fruit fly),chrysopsspp. (deerfly),cochliomyiaspp. (screw worm fly larva),contariniaspp. (midge),culexspp. (mosquito),dasineuraspp. (midge),Dasineura brassicae(cabbage midge),deliaspp.,Delia platura(seedcorn maggot),drosophilaspp. (vinegar fly),fanniaspp. (housefly),Fannia canicularis(little house fly),fanniascalaris (latrine fly),Gasterophilus intestinalis(nit fly),Gracillia perseae, Haematobia irritans(horn fly),hylemyiaspp. (root maggot),Hypoderma lineatum(common cattle grub),liriomyzaspp. (leaf miner),Liriomyza brassica(serpentine leafminer),Melophagus ovinus(sheep ked),muscaspp. (muscid fly),Musca autumnalis(face fly),Vusca domestica(house fly),Oestrus ovis(sheep bot fly),Oscinella frit(Sweden wheat stem maggot),Pegomyia betae(beet leafminer),phorbiaspp.,Psila rosae(carrotrust fly),Rhagoletis cerasi(cherry fruit fly),Rhagoletis pomonella(apple maggot),Sitodiplosis mosellana(orange wheat blossom midge),Stomoxys calcitruns(stable fly),tahanusspp. (horse botfly) andtipulaspp. (daddy-longlegs).

Hemiptera (stink bug),Acrosternum hilare(green stink bug),Blissus leucopterus(chinch bug),Calocoris norvegicus(potato mirid),Cimex hemipterus(tropical bed bug),Cimex lectularius(bed hug),Daghertus fasciatus, Dichelops furcatus, Dysdercus suturellus(cotton stainer),Edessa meditabunda, Eurygaster maura(cereal bug),Euschistus heros, Euschistus servus(brown stink bug),Helopeltis antonii, Helopeltis theivora(tea blight plantbug),lagynotomusspp. (stink bug),Leptocorisa oratorius, Leptocorisa varicornis, lygusspp. (plant bug),Lygus hesperus(western tarnished plant bug),Maconellicoccus hirsutus, Neurocolpus longirostris, Nezara viridula(southern green stink bug),PhyLocorisspp. (fleahopper),Phytocoris californicus, Phytocoris relativus, Piezodorus guildingi, Poecilocapsus lineatus(fourlined plant bug),Psallus vaccinicola, Pseudacysta perseae, Scaptocoris castaneaandtriatomaspp. (bloodsuckingconenose bug/kissing bug).

Homoptera (aphid, scale insect, whitefly and leafhopper):acrythosiphonpisum(pea aphid),adelgesspp. (adelgids),Aleurodes proletella(cabbage whitefly),Aleurodicus disperses, Aleurothrixus flccosus(woolly whitefly),aluacaspisspp.,Amrasca bigutella bigutella, aphrophoraspp. (leafhopper),Aonidiella aurantii(California red scale),aphisspp. (aphid),Aphis gossypii(cotton aphid),Aphis pomi(apple aphid),Aulacorthitm solani(foxglove aphid),bemisiaspp. (whitefly),Bemisia argentifolii, Bemisia tabaci(sweetpotato whitefly),Brachycolus noxius(Russian aphid),Brachycorynclia asparagi(asparagus aphid),Brevennia rehi, Brevicoryne brassicae(cabbage aphid),ceroplastesspp. (scale insect),Ceroplastes rubens(red wax scale),chionaspisspp. (scale insect),chrysomphalusspp. (scale insect),coccusspp. (scale insect),Dysaphis plantaginea(rosy apple aphid),empoascaspp. (leafhopper),Eriosoma lanigerum(woolly apple aphid),Icerya purchasi(cottony cushion scale),Idioscopus nitidulus(mango leafhopper),Laodelphax striatellus(smaller brown planthopper),Lepidosaphesspp.,Macrosiphumspp.,Macrosiphum euphorbiae(potato aphid),Macrosiphum granarium(English grain aphid),Macrosiphum rosae(rose aphid),Macrosteles quadrilineatus(aster leafhopper),Mahanarva frimbiolata, Metopolophium dirhodum(rose grain aphid),Midis longicornis, Myzus persicae(green peach aphid),Nephotettixspp. (leafhopper),Nephotettix cinctipes(green leafhopper),Nilaparvata lugens(brown planthopper),Parlatoria pergandii(chaff scale),Parlatoria ziziphi(ebony scale),Peregrinus maidis(corn delphacid),philaenusspp. (spittle insect),Phylloxera vitifoliae(grapephylloxera),Physokermes piceae(spruce bud scale),planococcusspp. (mealybug),pseudococcusspp. (mealybug),Pseudococcus brevipes(pine apple mealybug),Quadraspidiotus perniciosus(san Jose scale),Rhapalosiphumspp. (aphid),Rhapalosiphum maida(corn leaf aphid),Rhapalosiphum padi(oatbird-cherry aphid),saissetiaspp. (scale insect),Saissetia oleae(black scale insect),Schizaphis graminum(greenbug),Sitobion avenge(English wheat aphid),Sogatella furcifera(white-backed planthopper),therioaphisspp. (aphid), toumeyella spp. (scale insect),toxopteraspp. (aphid),trialeurodesspp. (whitefly),Trialeurodes vaporariorum(greenhouse whitefly),Trialeurodes abutiloneus(bandedwing whitefly),unaspisspp. (scale insect),Unaspis yanonensis(arrowhead scale) andZulia entreriana.

Hymenoptera (ant, wasp and bee):acromyrrmexspp.,Athalia rosae, attaspp. (leafcutting ants),camponotusspp. (carpenter ant),diprionspp. (sawfly),formicaspp. (ant),Iridomyrmex humilis(argentineant),monomoriumssp.,Monomorium minumum(little black ant),Monomorium pharaonis(pharaoh ant),neodiprionspp. (sawfly),pogonomyrmexspp. (harvest ant),polistesspp. (paper wasp),solenopsisspp. (fire ant),Tapoinoma sessile(odorous house ant),tetranomoriumspp. (pavement ant),vespulaspp. (yellow jacket) andxylocopaspp. (carpenter bee).

Isoptera (termite):coptotcrmcsspp.,Coptotermes curvignathus, Coptotermes frenchii, Coptotermes formosanus(formosan subterranean termite),cornitermesspp. (nasute termite),cryptotermesspp. (dry wood termite),heterotermesspp. (desert subterranean termite),Iieterotermes aureus, kalotermesspp. (dry wood termite),incistitermesspp. (dry wood termite),macrotermesspp. (fungus growing termite),marginitermesspp. (dry wood termite),microcerotermesspp. (harvester termite),Microtermes obesi, procornitermesspp.,reticulitermesspp. (limicolous termite),Reticulitermes banyulensis, Reticulitermes grassei, Reticulitermes flavipes(eastern limicolous termite),Reticulitermes hageni, Reticulitermes hesperus(western limicolous termite),Reticulitermes santonensis, Reticulitermes speratus, Reticulitermes tibialis, Reticulitermes virginicus, schedorhinotermesspp. andzootermopsisspp. (rottenwood termite).

Lepidoptera (moth and butterfly):Achoea janata, adoxophyesspp.,Adoxophyes orana, agrotisspp. (wireworm),Agrotis ipsilon(black wireworm),Alabama argillacea(cotton leafworm),Amorbia cuneana, Amyelosis transitella(navel orangeworm),Anacamptodes defectaria, Anarsia lineatella(peach twig borer),Anomis sabulijera(jute looper),Anticarsia gemmatalis(velvetbean caterpillar),Archips argyrospila(fruit tree leafroller),Archips rosana(rose leaf roller),argyrotaeniaspp. (tortricid moths),Argyrotaenia citrana(orange tortrix),Autographa gamma, Bonagota cranaodcs, Borbo cinnara(rice leaf folder),Bucculatrix thurberiella(cotton leafperforator),caloptiliaspp. (leaf miner),Capua reticulana, Carposina niponensis(peach fruit moth),chilospp.,Chlumetia transversa(mango shoot borer),Choristoneura rosaceana(oblique banded leaf roller),chrysodeixisspp.,Enaphalocerus medinalis(grass leafroller),coliasspp.,Conpomorpha cramerella, Cossus cossus(wood stupid moths),crambusspp. (sod webworms),Cydia funebrana(plum fruit moth),Cydia molesta(oriental fruit moth),Cydia nignicana(pea moth),Cydia pomonella(codling moth),Darna diducta, diaphaniaspp. (stem borer),diatraeaspp. (stalk bor er),diatraea saccharalis(sugarcane borer),Diatraea graniosella(southwester corn borer),eariasspp. (cotton bollworm),Earias insulata(Egyptian bollworm),Earias vit.ella(rough northern bollworm),Ecdytopopha aurantianum, Elasmopalpus lignosellus(lesser cornstalk borer),Epiphysias postruttana(light brown apple moth),ephestiaspp. (pink moth),Ephestia cautella(almond moth),Ephestia elutella(tobbaco moth),Ephestia kuehniella(mediterranean flour moth),epimecesspp.,Epinotia aporema, Erionota thrax(banana skipper),Eupoecilia ambiguella(grape berry moth),Euxoa auxiliaris(army cutworm),feltiaspp. (wireworm),gortynaspp. (stem borer),Grapholita molesta(peach(apricot)(oriental fruit moth),Hedylepta indicata(bean leaf webber),Helicoverpaspp. (noctuid),Helicoverpa armigera(cotton bollworm),Helicoverpa zea(corn borer(moth/cotton bollworm)),heliothisspp. (noctuid),Heliothis virescens(tobacco budworm),Hellula undalis(cabbage webworm),indarblaspp. (root moth),Keiferia lycopersicella(tomato pinworm),Leucinodes orbonalis(eggplant fruit borer),Leucoptera malifoliella, lithocollectisspp.,Lobesia botrana(grape fruit moth),loxagrotisspp. (noctuid),Loxagrotis albicosta(western bean cutworm),Lymantria dispar(gypsy moth),lyonetiaclerkella)(apple leafminer),mahasena corbetti(oil palm bagworm),malacosomaspp. (tent caterpillars),Mamestra brassicae(cabbage armyworm),Maruca testulalis(Maruca vitrata),Metisa plana(bagworm),Mythimna unipuncta(true armyworm),Neoleucinodes elegantalis(small tomato borer),Nymphula depunctalis(rice caseworm),Operophthera brumata(winter moth),Ostrinia nubilalis(European corn borer),Oxydia vesulia, Pandemis cerasana(common currant tortrix),Pandemis heparana(brown apple tortrix),Papilio demodocus, Pectinophora gossypiella(pink bollworm),peridromaspp. (wireworm),Peridroma saucia(variegated cutworm),Perileucoptera coffeella(white coffee leafminer),Phthorimaea operculella(potato tuber moth),Phyllocnisitis citrella, phyllonorycterspp. (leaf miner),Pieris rapae(imported cabbageworm),Plathypena scabra, Plodia interpunctella(Indian meal moth),Plutella xylostella(diamondback moth),Polychrosis viteana(grape berry moth),Prays endocarps, Prsys oleae(olive moth),pseudaletiaspp. (noctuid),Pseudaletia unipunctata(armyworm),Pseudoplusia includens(soybean looper),Rachiplusia nu, Scirpophaga incertulas, sesamiaspp. (stem borer),Sesamia inferens(pink rice stemborer),Sesamia nonagrioides, Setora nitens, Sitotroga cerealella(angoumois grain moth),Sparganothis pilleriana, spodopteraspp. (armyworm),Spodoptera exigua(beet armyworm),Spodoptera fugiperda(fall armyworm),Spodoptera oridania(southern armyworm),synanthedonspp. (root moth),Thecla basilides, Thermisia gemmatalis, Tineola bisselliella(webbing clothes moth),Trichoplusia ni(cabbage looper),Tuts absoluta, yponomeutaspp.,zeuzeracoffeae(red branch borer) andZeuzera pyrina(leopard moth).

Mallophaga (chewing lice):Bovicola ovis(sheep biting louse),Menacanthus stramineus(chicken body louse) andMenopon gallinea(common hen house).

Orthoptera (grasshopper, locust and cricket):Anabrus simplex(mormon cricket),gryllotalpidae(mole cricket),Locusta migratoria, melanoplusspp. (grasshopper),Microcentrum retinerve(angular winged katydid),pterophyllaspp. (katydid),Chistocerca gregaria, Scudderia furcata(fork tailed bush katydid) andValanga nigricorni.

Phthiraptera (sucking louse):haematopinusspp. (ox louse and pig louse),Linognathus ovillus(sheep louse),Pediculus humanus capitis(body louse),Pediculus humanus humanus(body louse) andPthirus pubis(crab louse).

Siphonaptera (flea):Ctenocephal ides canis(dog flea),Ctenocephalides felis(cat flea) andPulex irritans(human flea).

Thysanoptera (thrips):Frankliniella fusca(tobacco thrip),Frankliniella occidentalis(western flower thrips),Frankliniella shultzei, Frankliniella williamsi(corn thrip),Iieliothrips haemorrhaidalis(greenhouse thrip),Riphiphorothrips cruentatus, scirtothripsspp,Scirtothrips cirri(citrus thrip),Scirtothrips dorsalis(yellow tea thrips),Taeniothrips rhopalantennalisandthripsspp.

Thysanura (bristletail):lepismaspp. (silverfish) andthermobiaspp. (special mess fish).

Acarina (mite and tick):Acarapsis woodi(tracheal mite of honeybee),acarusspp. (food mites),Acarus siro(grain mite),Aceria mangiferae(mango bud mite),aculopsspp.,Aculops lycopersici(tomato russet mite),Aculops pelekasi, Aculus pelekassi, Aculus schlechtendali(apple rust mite),Amblyomma amcricanum(lone star tick),boophilusspp. (tick),Brevipalpus obovatus(privet mite),Brevipalpus phoenicis(red and black flat mite),demodexspp. (mange mites),dermacentorspp. (hard tick),Dermacentor variabilis(American dog tick),Dermatophagoides pteronyssinus(house dust mite),eotetranycusspp.,Eotetranychus carpini(yellow spider mite),epitimerusspp.,eriophyesspp.,ixodes(tick),metatetranycusspp.,Notoedres cati, oligonychusspp.,Oligonychus coffee, Oligonychus ilicus(southernred mite),panonychusspp.,Panonychus cirri(citrus red mite),Panonychus ulmi(European red mite),Phyllocoptruta oleivora(citrus rust mite),Polyphagotarsonemun latus(broad mite),Rhipicephalus sanguineus(brown dog tick),rhizoglyphusspp. (bulb mite),Sarcoptes scabiei(itch mite),Tegolophus perseaflorae, tetranychusspp.,Tetranychus urticae(twospotted spider mite) andVarroa destructor(bee mite).

Nematoda (nematode):aphelenchoidesspp. (bud and leaf & pine wood nematode),belonolaimusspp. (sting nematodes),criconemellaspp. (ring nematodes),Dirofilaria immitis(dog heartworm),ditylenchusspp. (stem and corm nematode),heteroderaspp. (cyst nematode),Heterodera zeae(corn cyst nematode),hirschmanniellaspp. (root nematodes),hoplolaimusspp. (lance nematodes),meloidogynespp. (knot nematode),Meloidogyne incognita(knot nematode),Onchocerca volvulus(hook-tail worm), praLylenchus spp. (lesion nematode),radopholusspp. (burrowing nematode) andRotylenchus reniformis(kidney-shaped nematode).

Symphyla (comprehensive insects):Scutigerella immaculata.

Due to the positive characteristics, the above compounds can be advantageously used to protect important crops, livestock and breeding stock in agriculture and horticulture, and to avoid the damage of fungi, pests and mites to the environment that humans often go to.

To achieve an ideal effect, the use amount of the compound varies depending on various factors such as the used compound, the crop to be protected, the type of pest, the degree of infection, climatic conditions, the method of administration, and the adopted dosage form.

The dose of 10 grams to 5 kilograms of compound per hectare can provide adequate control.

The present invention also comprises a fungicidal, insecticidal and acaricidal composition using the compound shown by the general formula I as an active ingredient. The weight percentage of the fungicidal, insecticidal and acaricidal composition in the active ingredient is 0.5-99%. The fungicidal, insecticidal and acaricidal composition also comprises acceptable carriers in agriculture, forestry and sanitation.

The composition of the present invention can be applied in the form of formulations. The compound shown by the general formula I is dissolved or dispersed in the carrier as the active ingredient or prepared into the formulation for easier dispersion when used as a fungicide and an insecticide. For example, the chemical formulations can be prepared into wettable powder, an oil dispersion, an aqueous suspension, an aqueous emulsion, a water aqua or missible oil.

In these compositions, one liquid or solid carrier is at least added, and appropriate surfactants may be added when required.

The technical solution of the present invention also comprises a method for controlling fungi, pests and mites: applying the fungicidal, insecticidal and acaricidal composition of the present invention to a fungi or a growth medium of the fungi. The more appropriate effective dose which is often selected is 10 to 1000 grams per hectare, and preferably, the effective dose is 20 to 500 grams per hectare.

For some applications, for example in agriculture, the addition of one or more other fungicides, insecticides, acaricides, herbicides, plant growth regulators or fertilizers to the fungicidal, insecticidal and acaricidal composition of the present invention can produce additional advantages and effects.

It should be clear that various changes and modifications can be made within the scope defined by the claims of the present invention.

The Present Invention has the Following Advantages:

The substituted pyrimidine compound shown by the general formula I of the present invention has obvious structural features, so that the compound has novel structure. Moreover, the compound of the present invention has obvious fungicidal, insecticidal and acaricidal activity, and has outstanding effect on different target crops. Meanwhile, under some different low dosages (e.g., 25 ppm, 10 ppm, 8.3 ppm, 6.25 ppm, 2.8 ppm and 2.5 ppm) part of the compounds of the present invention have outstanding effects, thereby reducing the utilization cost. Further, it can be seen that the compound shown by the general formula I in the present invention shows excellent activity against various fungi in agriculture or other fields, also shows good activity against pests and mites, and can be further developed into a new fungicide, insecticide and acaricide.

