Research Progress of Trifluoromethylation with Sodium Trifluoromethanesulfinate

Abstract

Trifluoromethyl can increase the chemical and metabolic stability of drugs, improve its lipophilicity and bioavailability, and furthermore, enhance drug binding selectivities. Sodium trifluoromethanesulfinate (CF3SO2Na) is a stable inexpensive reagent, which has been widely used in the field of organic fluorine chemistry. The recent progress (2014~2017) in trifluoromethylation by employing CF3SO2Na as the trifluoromethyl source is summarized. In addition, the reactions of bifunctionalization, trifluoromethylation of aromatics, trifluoromethylthioization and other types of reactions are described respectively, with their applications and reaction mechanism. It is hoped that this review can be referred to in the studies of trifluoromethyl introduction.