Copper-Catalyzed, Intramolecular Amination of Unactivated C(sp)-H Bonds through Radical Relay.

Although copper-catalyzed amination of activated C(sp)-H bonds through radical relay has been developed, amination of unactivated C(sp)-H bonds is rare. Herein, copper-catalyzed intramolecular amination of remote unactivated C(sp)-H bonds is reported. The reaction is conducted in a mild and effective manner with moderate to good yields, demonstrating broad tolerance toward various functional groups and exhibiting complete regio- and chemoselectivities. This innovation supplies novel synthetic pathways for the construction of saturated nitrogenated heterocycles.