Pd-catalyzed CH (phenylsulfonyl)difluoromethylation of electron-rich heteroarenes

Abstract

A novel Pd(0)-catalyzed CH (phenylsulfonyl)difluoromethylation of electron-rich heteroarenes has been developed. The reaction utilizing PhSO₂CF₂I as a (phenylsulfonyl)difluoromethylation reagent proceeds efficiently. Mechanistic studies indicate that the CH (phenylsulfonyl)difluoromethylation occurs via a radical pathway. This method demonstrates broad substrate compatibility, including a variety of heterocycles containing nitrogen, oxygen, and sulfur atoms, achieving excellent yields. This study provides an efficient and versatile approach for synthesizing (phenylsulfonyl)difluoromethylated heterocycles, which are valuable in pharmaceuticals, agrochemicals, and materials. The mild reaction conditions and high efficiency of this method make it a promising tool for expanding the scope of organofluorine chemistry applications.