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A ZnCl 2 -catalyzed diastereoselective Joullié-Ugi three-component reaction from 2 H-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.

the journal of organic chemistry

Lewis Acid-Catalyzed Diastereoselective Synthesis of Multisubstituted <i>N</i>-Acylaziridine-2-carboxamides from 2<i>H</i>-Azirines via Joullié–Ugi Three-Component Reaction

Lewis Acid-Catalyzed Diastereoselective Synthesis of Multisubstituted N-Acylaziridine-2-carboxamides from 2H-Azirines via Joullié–Ugi Three-Component Reaction