Palladium‐Catalyzed anti‐Markovnikov Halosulfonamidation of Unactivated Alkene†

Abstract

Comprehensive SummaryPalladium‐catalyzed regioselective amination of unactivated alkene remains a challenge and is of great interest. Herein, a three‐component coupling of unactivated alkene, sulfonamide, and N‐halo compounds accessing vicinal haloamine has been conceived. This aminohalogenation represents a modular and regioselective strategy. The electrophilic halogenating agent enables regioselective anti‐Markovnikov aminopalladation and facilitates subsequent halogenation events. And this protocol is characterized by gram‐scale syntheses and late‐stage functionalizations. Of note, the recovered byproduct phthalimide allows for reusing by conversion to the starting material.