Cu(I)-Catalyzed [2 + 2 + 1] Cycloaddition of Amines, Alkynes, and Ketenes: An Umpolung and Regioselective Approach to Full-Substituted β-Pyrrolinones.

Described here is a Cu-catalyzed [2 + 2 + 1] modular synthesis of full-substituted β-pyrrolinones from simple amines, alkynes, and α-diazo-β-ketoesters. This approach involving the regioselective C-nucleophilic attack of enamines, uncommon C-nucleophilic addition to ketenes, and umpolung of imines enables the direct synthesis of full-substituted β-pyrrolinones, which were hardly constructed by traditional synthetic strategies.