Copper-Catalyzed Enantioselective Intramolecular Aryl C-N Coupling: Synthesis of Enantioenriched 2-Oxo-1,2,3,4-tetrahydroquinoline-3-carboxamides via an Asymmetric Desymmetrization Strategy

The differentiation of two nucleophilic amide groups in malonamides through a copper-catalyzed enantioselective intramolecular aryl C-N coupling reaction is demonstrated based on an asymmetric desymmetrization strategy. Such a method afforded enantioenriched 2-oxo-1,2,3,4-tetrahydroquinoline-3-carboxamides in high yields and moderate to good enantioselectivity.