Abstract

Although copper-catalyzed amination of activated C(sp3)-H bonds through radical relay has been developed, amination of unactivated C(sp3)-H bonds is rare. Herein, copper-catalyzed intramolecular amination of remote unactivated C(sp3)-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.

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