Photoinduced Metal-/Additive-Free Difluoromethylation of N-Heteroaromatics†

Abstract

Herein, we report a photo-induced, metal-/additive-free protocol for the difluoromethylation of N-heteroaromatics with [bis(difluoroacetoxy)iodo]benzene as the difluoromethylation reagent. The protocol affords difluoromethylated N-heteroaromatics in moderate to good yield (up to 91%). The transformation is compatible with a wide range of substrates and has good tolerance towards various functional groups. Moreover, the synthetic value of this method is further demonstrated by applications in gram-scale synthesis and the late-stage functionalization of biologically important molecules.