Chiral butyrolacto[3,4-b]-2(S)-6(R)-1-N-akylaziridines 7 were synthesized in enantiopure form utilizing racemic 5-methoxy-3-bromo-2(5H)-furanone (5) and available amines (6) as key precursors. After highly effective reduction of 7, the functionalized 2(S),3(R)-dihyroxymethyl-N-alkylaziridines (8) were obtained in good yields with ≥98% ee. This is a simple and pratical method for the preparation of enantiopure aziridines which are important interme-diates in the synthesis of biologic active molecules. Chiral butyrolacto [3,4-b] -2 (S) -6 (R) -1-N-akylaziridines 7 were synthesized in enantiopure form utilizing racemic 5-methoxy- After efficient cure of 7, the functionalized 2 (S), 3 (R) -dihyroxymethyl-N-alkylaziridines (8) were obtained in good yields with ≥98% ee. This is a simple and pratical method for the preparation of enantiopure aziridines which are important interme-diates in the synthesis of biologic active molecules.