Cu-Catalyzed Remote Transarylation of Amines via Unstrained C-C Functionalization

Remote arylation of amines via C-C bond functionalization has not been reported yet. Herein, we develop the gamma-transarylation of amines through the cleavage of unstrained C-C bond enabled by copper catalysis under mild conditions, representing the example of utilization of unstrained C-C bond for metal-catalyzed C-C cross-coupling. Mechanistic investigations reveal that the redox-neutral reaction undergoes an intercepted radical pathway to cleave the C-sp2-C-sp3 bond, followed by the combination with copper-catalyzed arylation reaction in the presence of aryl boronic acid to construct a new C-sp2-C-sp3 bond.