Recent Advances in Difluoromethylthiolation

Abstract

The difluoromethylthio group (HCF2S), which has been identified as a valuable functionality in drug and agrochemical discovery, has received increased attention recently. Two strategies, difluoromethylation and direct difluoromethylthiolation, have been well established for HCF2S incorporation. The former strategy suffers from the need to prepare sulfur-containing substrates. In contrast, direct difluoromethylthiolation is straightforward and step-economic. This short review covers the recent advances in direct difluoromethylthiolation, including electrophilic, radical, and transition-metal-catalyzed or -promoted reactions­. 1 Introduction 2 Electrophilic Difluoromethylthiolation 3 Radical Difluoromethylthiolation 4 Transition-Metal-Catalyzed or -Promoted Difluoromethylthiolation 5 Conclusions and Perspectives