Difluoromethylthiolation of Phenols and Related Compounds with a HFCSONa/PhPCl/MeSiCl System.

A novel HFCSONa/PhPCl/MeSiCl system is disclosed for the late-stage direct difluoromethylthiolation of C and C nucleophiles. Difluoromethylthiolation of phenols and naphthols proceeded nicely under this system to regioselectively provide corresponding SCFH compounds in good yields. Other substrates such as indoles, pyrroles, pyrazoles, enamines, ketones, and β-keto esters were also transformed to corresponding SCFH products in good yields. The late-stage direct difluoromethylthiolation of a number of natural products and pharmaceutically attractive molecules was also achieved.