A convenient three-component tetrafluoroethylation reaction of alkenes induced by visible light has been developed using 1,1,2,2-tetrafluoroethylsulfonyl chloride and quinoxalin-2(1H)-ones. This method provides a facile approach to introduce the HCF₂CF₂ group into organic molecules under mild conditions, enabling the late-stage modification of biologically active and drug molecules.

Abstract

1,1,2,2-Tetrafluoroethyl-containing compounds are valuable structures due to their unique physicochemical properties, which have increasing potential application in drug discovery. However, synthetic methods for preparing such compounds are rare. Herein, we report the first use of 1,1,2,2-tetrafluoroethanesulfonyl chloride to introduce the HCF₂CF₂ group into organic molecules via a three-component, radical tetrafluoroethyl-heteroarylation of alkenes with readily available quinoxalin-2(1H)-ones. This method provides a new and facile approach for late-stage functionalization of potential biologically active molecules.