Studies Towards the Synthesis of the Core of Endiandric Acid H
In the presence of a CuBr·SMe2 catalytic system, a very simple and efficient approach for the synthesis of the key precursor of the core of endiandric acids starting from the readily and abundantly available 3-butyn-1-ol in five linear steps with an overall yield of 40% was developed.
Synthesis and antifungal activity of novel chiral indole analogues.
Starting from L-tryptophan, 19 new N-substituted chiral indole analogs were synthesized. The prepared compounds were evaluated for biological activity against Sclerotinia sclerotiorum, Alternaria solani, Verticillium dahliae, Colletotrichum orbiculare, Cytospora juglandis and Curvularia lunata. The preliminary bioassays showed that most of the synthesized compounds exhibited fungicidal activity. Compound b13 in particular exhibited significant antifungal activity against Verticillium dahliae and Sclerotinia sclerotiorum, with the MIC value of 1.95 µg mL-1. Compound b13 also showed excellent activity against six plant pathogen fungi, and was identified as the most active on the biological assays, and will be studied further.
Catalytic removal of tert-butyldimethylsilyl (TBS) ether by PVP-I
Abstract A mild, efficient and rapid protocol the deprotection of alcoholic TBDMS ethers using PVP-1 as catalyst in methanol, the procedure of deprotection of various TBDMS ethers were found to be very convenient, easy work-up, high yielding.