Copper‐Catalyzed Electrophilic Amination of Heteroarenes and Arenes by CH Zincation

Abstract Direct amination of heteroarenes and arenes has been achieved in a one‐pot CH zincation/copper‐catalyzed electrophilic amination procedure. This amination method provides an efficient and rapid approach to access a diverse range of heteroaromatic and aromatic amines including those previously inaccessible using CH amination methods. The mild reaction conditions and good functional‐group compatibility demonstrate its great potential for the synthesis of important and complex amines.