Cu‐Catalyzed C(sp2)−H Bond Aminosulfonylation of Maleimides

Abstract A copper‐catalyzed direct C( sp 2 )−H bond aminosulfonylation of maleimides is demonstrated. This protocol enables concurrent construction of C( sp 2 )−N and C( sp 2 )−SO 2 bonds in one‐step and features high efficiency, broad substrate scopes, good functional‐group tolerance, and mild reaction conditions. Preliminary mechanistic studies indicate that the reaction probably involves a radical way. Significantly, this method is applicable to synthesize derivatives of pharmaceuticals such as Desloratadine, Fluoxetine, Atomoxetine, and Maprotiline.