手性氮丙啶试剂的合成

L－缬氨酸和L－异亮氨酸经NaBH4还原得到相应的氨基醇化合物1（a,b）；再经与对甲苯磺酰氯反应得到3－甲基－2－对甲苯磺酰氨基－丁醇对甲苯磺酸酯2a和3－甲基－2－对甲苯磺酰氨基－戊醇对甲苯磺酸酯2b；化合物2(a,b）在强碱条件下经环化反应得两种手性氮丙试剂3a和3b，对中间体2的合成条件进行了探讨，并测定了手性氮丙啶试剂的旋光性，所有中间体和手性氮丙啶试剂均经元素分析、^1HNMR,MS等证实了它们的结构和组成。

Syntheses of Chiral Aziridine Reagents

L-Valinol (1a) and L-Isoleucinol (1b) were synthesized by the reaction of L-Valine and L-Isoleucine with NaBH 4, respectively. The reaction of 1a and 1b with TsCl gave 3-methyl-2-tosylamino-butanol-tosylate(2a) and 3-methyl-2-tosylamino-petanol-tosylate(2b), respectively. The cyclination of 2a and 2b in the presence of KOH obtained chiral aziridine reagents 3a and 3b, respectively. The synthetic condition of intermediates 2 was studied. The rotatory characteristic of 3a,b was measured. All intermediates and chiral aziridines were identified by elemetal analysis, 1H NMR and MS.;