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抗痛风药非布索坦的合成工艺优化
引用本文:姚刚,杨威.抗痛风药非布索坦的合成工艺优化[J].化学与生物工程,2012,29(12):75-79.
作者姓名:姚刚  杨威
作者单位:湖北科技学院药学院,湖北咸宁,437100
摘    要:以2-(3-甲酰基-4-异丁氧基一苯基)-4-甲基-噻唑-5-甲酸乙酯为原料,经醛肟脱水、水解制备非布索坦,并对其工艺进行了优化。合成的非布索坦纯度达到99%以上,单个杂质不超过0.1%,总收率达63.31%。优化后的工艺简单易控,产品纯度及收率较高,达到药用标准。

关 键 词:非布索坦  抗痛风药  工艺优化

Optimization of Synthetic Process of Anti-Gout Drug Febuxostat
YAO Gang , YANG Wei.Optimization of Synthetic Process of Anti-Gout Drug Febuxostat[J].Chemistry & Bioengineering,2012,29(12):75-79.
Authors:YAO Gang  YANG Wei
Affiliation:(School of Pharmacy,Hubei University of Science and Technology,Xianning 437100,China)
Abstract:With ethyl 2-(3-formyl-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylate as raw material, fe- buxostat was synthesized through the hindered dehydration and the latter hydrolysis reaction,and the process was optimized. The febuxostat was obtained with purity over 99% ,single impurity not exceeding 0.1% and to- tal yield, 63.31%. The optimized process was simple and easy to control with high purity and yield, the product met the requirement of medical standard.
Keywords:febuxostat i anti-gout drugl process optimization
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