Rhodium(III)-Catalyzed Amidation of Unactivated C(sp3)H Bonds

Nitrogenation by direct functionalization of CH bonds represents an important strategy for constructing CN bonds. Rhodium(III)-catalyzed direct amidation of unactivated C(sp(3))H bonds is rare, especially under mild reaction conditions. Herein, a broad scope of C(sp(3))H bonds are amidated under rhodium catalysis in high efficiency using 3-substituted 1,4,2-dioxazol-5-ones as the amide source. The protocol broadens the scope of rhodium(III)-catalyzed C(sp(3))H activation chemistry, and is applicable to the late-stage functionalization of natural products.