While radical addition to SO 2 serves as a fundamental strategy for constructing sulfone frameworks, its application in building sulfonamide skeletons, particularly for the modular installation of an aminosulfonyl moiety across alkene substrates, remains underdeveloped. Herein, we report unprecedented photocatalytic intermolecular 1,2-difluoromethylation/ aminosulfonylation of unactivated alkenes employing commercially available, bench-stable CF 2 HSO 2 Na as a bifunctional reagent and O-Ts hydroxylamine as electrophilic aminating reagents. The protocol demonstrates broad substrate scope and exceptional functional group tolerance, enabling the late-stage functionalization of complex pharmaceuticals. Mechanistic investigations support radical-polar crossover processes. This work provides a novel, efficient, and environmentally benign strategy for constructing valuable β -difluoromethylated sulfonamide scaffolds, aligning with core principles of green synthesis. We report unprecedented photocatalytic intermolecular 1,2-difluoromethylation/aminosulfonylation of unactivated alkenes employing commercially available, bench-stable CF 2 HSO 2 Na as a bifunctional reagent and O-Ts hydroxylamine as electrophilic aminating reagents.
Dong et al. (Sun,) studied this question.
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