Copper-Catalyzed Aerobic Oxidative Amination of sp3C-H Bonds: Efficient Synthesis of 2-Hetarylquinazolin-4(3H)-ones

An efficient synthesis of 2-hetarylquinazolin-4(3H)-ones via copper-catalyzed direct aerobic oxidative amination of sp(3)C-H bonds has been developed. This tandem oxidation-amination-cyclization transformation represents a straightforward protocol to prepare 2-hetaryl-substituted quinazolinones from easily available 2-aminobenzamides and (2-azaaryl)methanes.