中文摘要：

手性元5-（R）-（1R，2S，5R）-孟氧基-3-溴-2（5H）-呋喃酮（3）与氮亲核试剂伯胺（4），通过串联的不对称Michael加成，分子内亲核取代反应得到了具有两个新的手性中心的1R，5S-6-烷基-6-氮杂-2R-孟氧基-3-氧杂-4-氧代二环[3，1，0]己烷（5a～5d），产率41％-51％，e．e．≥98％．后者经LiAlH4还原得到N-烷基-2，3-双（羟甲基）氮杂环丙烷（6a-6d），产率66％-91％．化合物5和6通过元素分析，IR，1^HNMR，13^CNMR，MS以及X射线晶体分析，测定了它们的化学结构及立体化学构型．本文为N-烷基氮杂环丙烷类化合物的合成提供了一种有效途径．

英文摘要：

The chiral 1R,5S-6-alkyl-6-aza-2R-menthoxy-3-oxa-4-oxobicyclo[3,1,0]hexane （5a-5d） containing two stereogenic centers were obtained in 41%-51% yields with e.e.≥98% via the tandem asymmetric Michael addition and internal nucleophilic substitution reaction of the chiron 3 with the primary amine 4 as a nucleophile. After the effective reduction of compounds 5 by LiAlH4 in THF, the target molecules, meso-N-alkyl-2,3-bis（hydroxymethyl）aziridines （6a-6d） were obtained in 66%-91% yields. The chemical structures of 5 and 6 were readily confirmed by analytical and spectroscopic data. The proposed structures of optically active compounds were consistent with the stereochemistry and configuration of their molecules further confirmed by the X-ray crystallography of 5a and 6c. These results could provide a new synthetic route to the functionalized optically active aziridine derivatives.