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手性合成(R)-2-羟基苯丁酸乙酯的研究
引用本文:刘昱,李翔,刘小成,何嘉俊,刘端.手性合成(R)-2-羟基苯丁酸乙酯的研究[J].化学与生物工程,2009,26(7):37-39.
作者姓名:刘昱  李翔  刘小成  何嘉俊  刘端
作者单位:湖北省化学研究院,湖北,武汉,430074
摘    要:(R)-2-羟基苯丁酸乙酯是合成普利类抗高血压药物的重要手性中间体.通过正交实验优化了(R)-2-羟基苯丁酸乙酯中间体2-氧代苯丁酸乙酯的合成,利用亚硫酸氢钠提纯,得到了纯度为98%的2-氧代苯丁酸乙酯;添加8-羟基喹啉来提高不对称氢化的选择性,可以提高产品e.e.值.

关 键 词:(R)-2-羟基苯丁酸乙酯  2-氧代苯丁酸乙酯  不对称氢化  提纯

Study on the Enantioselective Synthesis of Ethyl(R)-2-hydroxy-4-phenylbutanate
LIU Yu,LI Xiang,LIU Xiao-cheng,HE Jia-jun,LIU Duan.Study on the Enantioselective Synthesis of Ethyl(R)-2-hydroxy-4-phenylbutanate[J].Chemistry & Bioengineering,2009,26(7):37-39.
Authors:LIU Yu  LI Xiang  LIU Xiao-cheng  HE Jia-jun  LIU Duan
Affiliation:Hubei Institute of Chemistry;Wuhan 430074;China
Abstract:Ethyl(R)-2-hydroxy-4-phenylbutanate is an important chiral intermediate for ACEI drugs.In this paper,orthogonal experiment was applied to optimize the synthesis of intermediate ethyl 2-oxo-4-phenylbutanate,and sodium bisulfite was used to obtain the intermediate with purity of 98%.8-Hydroxyquinoline was added to improve the selectivity of asymmetric hydrogenation and it was found that the e.e.value of the product was enhanced.
Keywords:ethyl(R)-2-hydroxy-4-phenylbutanate  ethyl 2-oxo-4-phenylbutanate  asymmetric hydrogenation  purification
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