[1]潘 璐,王晓东,纪九胜.缬沙坦苄酯的水解反应工艺[J].常州大学学报(自然科学版),2012,(01):14-17.
　PAN Lu,WANG Xiao-dong,JI Jiu-sheng.Study of Hydrolysis Process of Valsartan Benzyl Ester[J].Journal of Changzhou University(Natural Science Edition),2012,(01):14-17.
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缬沙坦苄酯的水解反应工艺()
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常州大学学报(自然科学版)[ISSN:2095-0411/CN:32-1822/N]

卷:
期数:
2012年01期
页码:
14-17
栏目:
出版日期:
2012-01-01

文章信息/Info

Title:
Study of Hydrolysis Process of Valsartan Benzyl Ester
作者:
潘 璐; 王晓东; 纪九胜
常州四药制药有限公司 原料药厂,江苏 常州 213004
Author(s):
PAN Lu; WANG Xiao-dong; JI Jiu-sheng
Pharmaceutical Ingredient Plant,Changzhou Siyao Pharmaceuticals Co.Ltd.,Changzhou 213004,China
关键词:
缬沙坦苄酯;  乙醇;  缬沙坦
Keywords:
valsartan benzyl ester;  ethanol;  valsartan
分类号:
TQ 314
文献标志码:
A
摘要:
以缬沙坦苄酯为原料,经水解反应合成了缬沙坦,对其结构进行了IR确证。考察了碱液浓度、反应温度、原料配比等因素对反应的影响,采用正交试验法对缬沙坦合成工艺进行了优化。结果表明,以乙醇为溶剂,碱浓度2.0 mol/L,n(缬沙坦苄酯):n(氢氧化钠)=1:8,反应温度40 ℃时,缬沙坦收率达71.5%,产品的化学纯度达99.90%,光学纯度达99.85%。
Abstract:
Valsartan was obtained by hydrolysis debenzylation of valsartan benzyl ester. The molecular structure of the product was confirmed by IR.The effects of different factors including alkali concentration, reaction temperature and raw material ratio on hydrolysis debenzylation were investigated. Theprocess conditions of the reaction were optimized by orthogonal experiments. The result showed that when alkali concentration was 2.0 mol/L, reaction temperature was 40 ℃,the ratio of n(valsartan benzyl ester)to n(NaOH)was 1:8, the target product yield reached 71.5% with a chemical purity of 99.90% and an optical purity of 99.85%.

参考文献/References:

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备注/Memo

备注/Memo:
作者简介:潘璐(1972-),男,江苏武进人,工程师。
更新日期/Last Update: 2012-01-01