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 beta-pyrrolinones from simple amines, alkynes, and alpha-diazo-beta-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 beta-pyrrolinones, which were hardly constructed by traditional synthetic strategies.

Automated summary

Described here is a Cu-catalyzed [2 + 2 + 1] modular synthesis of full-substituted beta-pyrrolinones from simple amines, alkynes, and alpha-diazo-beta-ketoesters. This approach enables the direct synthesis of full-substituted beta-pyrrolinones, which were hardly constructed by traditional synthetic strategies.