Copper-Catalyzed Electrophilic Amination of Heteroarenes via C–H Alumination

A highly efficient Cu-catalyzed electrophilic amination reaction of readily available heteroarenes with O-benzoyl hydroxylamines via a one-pot C–H alumination is reported. The reactions were catalyzed using 1 mol % of CuCl to afford various heteroaryl amines in good to excellent yields. The direct C–H lithiation/transalumination of heteroarenes and catalytic amination sequence can be performed in a single vessel on gram scales.