Enantioselective Copper-Catalyzed Intramolecular N−H Bond Insertion: Synthesis of Chiral 2-Carboxytetrahydroquinolines

The first highly enantioselective intramolecular N−H bond insertion was realized by using copper catalysts modified with chiral spirobisoxazoline ligands, which provides a novel strategy for the synthesis of chiral 2-carboxytetrahydroquinolines. This reaction features fast reaction rate, high yield, high enantioselectivity, and mild reaction conditions.