Copper-Catalyzed C-N Bond Formation via Oxidative Cross-Coupling of Amines with α-Aminocarbonyl Compounds

A novel and selective method for the simple copper-catalyzed alpha-amination of alpha-aminocarbonyl compounds to afford 2-amino-2-iminocarbonyl and 2-amino-2-oxocarbonyl compounds is reported. This transformation is achieved by C(sp3)-H and N-H bond oxidative cross-coupling and selective C-N bond oxidative cleavage. This reaction system has a broad reaction scope, providing a facile pathway for the alpha-functionalization of alpha-amino ketones.