Biodistribution of 6-[211At]astato-2-methyl-1,4-naphthoquinol bis(diphosphate salt) and 211At- in mice with a transplanted rectal adenocarcinoma.
6-[211At]astato-MNDP is currently being investigated as a potential high LET endoradiotherapeutic drug. Biodistribution and whole-body radiation retention studies have been carried out with 6-[211At]astato-MNDP and 211At- in a murine rectal tumour model; results indicate that the 211At-C bond in the compound is metabolically stable for at least 6 h. The Mean Biological Concentration of 6-[211At]astato-MNDP in tumour tissue ranged from 170-253% over an initial 12 h period; this was higher than that observed for the [211At]astatide anion. Conversely, the uptake of compound into radiobiologically critical organs was significantly lower.
6-211At-Astato-2-methyl-1,4-naphthoquinol bis (disodium phosphate): A novel α-emitting potential anti-tumour drug
6-211At-Astato-2-methyl-1,4-naphthoquinol bis (disodium phosphate) has been prepared as a potential endoradiotherapeutic drug for metastatic malignant disease. Astatine-211 was introduced into the unsubstituted aromatic ring of 2-methyl-1,4-naphthoquinone via the 6-chloromercuriderivative; the 5-stage synthesis was completed within one half-life. Overall radiochemical efficiency ranged from 28–32%, with a specific activity 3.5–3.7 μCi μmol−1 from 200 μCi 211At.
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.