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

A multicomponent organocatalyzed highly diastereo- and enantioselective synthesis of CF3-substituted aziridines is described. This reaction of in situ generated CF3HN2 and aldimines was realized by chiral Bronsted acid catalysis. The utility of the products is illustrated by easy access to beta-CF3 isocysteine and aziridine-containing dipeptides.