Lewis acid-catalyzed diastereoselective synthesis of multisubstituted N-acylaziridine-2-carboxamides from 2 H -Azirines via Joullié-Ugi three-component reaction
A ZnCl2-catalyzed diastereoselective Joullié-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.
Angyal, Anikó,Demjén, András,Wéber, Edit,Kovács, Anita K.,W?lfling, János,Puskás, László G.,Kanizsai, Iván