Copper-Catalyzed Intramolecular Amination of C(sp3)–H Bond of Secondary Amines to Access Azacycles

The cross-coupling of C–N bond directly from inert C–H bonds is an ideal approach to synthesize saturated azacycles due to its high efficiency and atom economy. In this article, a copper-catalyzed intramolecular amination via the cross coupling of C(sp3)–H and N–H bonds of secondary amine has been reported, which exhibit excellent chemo- and regioselectivity, extensive substrate scope, and functional group tolerance in good to excellent yield, offering an efficient pathway to build nitrogen-containing heterocycle skeletons.