Lewis Acid-Catalyzed Diastereoselective Synthesis of Multisubstituted N-Acylaziridine-2-carboxamides
from 2H-Azirines via Joullie-Ugi Three-Component Reaction
A ZnCl2-catalyzed diastereoselective Joullie Ugi three-component reaction from 2H-azirines,
isocyanides, and carboxylic acids was established. The protocol allows the preparation
of highly and diversely functionalized N-acylaziridine-2-carboxamide derivatives in
up to 82% isolated yields. Moreover, the applicability of N-acylaziridines is demonstrated
through a variety of transformations.