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有机化学
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有机化学 ›› 2003, Vol. 23 ›› Issue (6): 542-545. 上一篇    下一篇

研究论文

手性（Salen)CO催化的末端环氧化合物水解动力学拆对反应在手性药物合成中的应用

沈凯圣;熊飞;胡娟;杨琍苹   

  1. 华东师范大学化学系
  • 发布日期:2003-06-25

Application of Chiral (Salen) Co-Catalyzed Hydrolytic Kinetic Resolution of Racemic Terminal Epoxides to the Syntheses of Chiral Drugs

Shen Kaisheng;Xiong Fei;Hu Juan;Yang Liping   

  1. Department of Chemistry,East China Normal University
  • Published:2003-06-25

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用手性(Salen)Co催化剂催化的外消旋末端环氧化合物的水解动力学拆分反应 所得的手性末端环氧化合物和各种取代的胺和烷氧负离子反应，可得到光学纯的β -胺基醇和β-烷氧基醇类化合物，这两类化合物是重要的生物活性分子．此方法应 用到手性药物T-588(治疗老年痴呆症药)和盐酸左旋沙丁胺醇(治疗哮喘药)的全合 成．

关键词: 钴, 催化剂, 环氧化物, 水解, 动力学, 盐酸左旋沙丁胺醇

The hydrolytic kinetic resolution (HKR) of racemic terminal epoxides catalyzed by chiral (salen)Co could afford optically active terminal epoxides. Chiralβ -amino alcohol and β-alkoxyl alcohol derivatives which are biologically important could be obtained by the ring-opening reactions of chiral terminal epoxides with amines and alkoxy anions. Application of this approach to the syntheses of chiral drugs, T-588 and (R)-albuterol is described.

Key words: COBALT, CATALYST, EPOXIDE, HYDROLYSIS, DYNAMICS, (R)-albuterol

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