化学与生物工程
化學與生物工程
화학여생물공정
CHEMISTRY & BIOENGINEERING
2009年
7期
37-39
,共3页
刘昱%李翔%刘小成%何嘉俊%刘端
劉昱%李翔%劉小成%何嘉俊%劉耑
류욱%리상%류소성%하가준%류단
(R)-2-羟基苯丁酸乙酯%2-氧代苯丁酸乙酯%不对称氢化%提纯
(R)-2-羥基苯丁痠乙酯%2-氧代苯丁痠乙酯%不對稱氫化%提純
(R)-2-간기분정산을지%2-양대분정산을지%불대칭경화%제순
ethyl(R)-2-hydroxy-4-phenylbutanate%ethyl 2-oxo-4-phenylbutanate%asymmetric hydrogenation%purification
(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.
(R)-2-羥基苯丁痠乙酯是閤成普利類抗高血壓藥物的重要手性中間體.通過正交實驗優化瞭(R)-2-羥基苯丁痠乙酯中間體2-氧代苯丁痠乙酯的閤成,利用亞硫痠氫鈉提純,得到瞭純度為98%的2-氧代苯丁痠乙酯;添加8-羥基喹啉來提高不對稱氫化的選擇性,可以提高產品e.e.值.
(R)-2-간기분정산을지시합성보리류항고혈압약물적중요수성중간체.통과정교실험우화료(R)-2-간기분정산을지중간체2-양대분정산을지적합성,이용아류산경납제순,득도료순도위98%적2-양대분정산을지;첨가8-간기규람래제고불대칭경화적선택성,가이제고산품e.e.치.
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.
