A Valuable Synthetic Route to the Enantiopure Functionalized N‐Substituted Aziridines

Abstract Chiral butyrolacto[3,4‐ b ]‐2(S)‐6( R )‐l‐N‐alkylaziridines 7 were synthesized in enantiopure form utilizing racemic 5‐methoxy‐3‐bromo‐2(5 H )furanone (5) and available amines (6) as key precursors. After highly effective reduction of 7, the functionalized 2( S ),3( R )‐dihydroxymethyl‐ N ‐alkylaziridines (8) were obtained in good yields with ≥98% ee . This is a simple and practical method for the preparation of enantiopure aziridines which are important intermediates in the synthesis of biologic active molecules.