Chiral Brønsted acid-catalyzed diastereo- and enantioselective synthesis of CF3-substituted aziridines

Abstract

A multicomponent organocatalyzed highly diastereo- and enantioselective synthesis of CF₃-substituted aziridines is described. This reaction of in situ generated CF₃CHN₂ and aldimines was realized by chiral Brønsted acid catalysis. The utility of the products is illustrated by easy access to β-CF₃ isocysteine and aziridine-containing dipeptides.