化工进展

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奥扎格雷合成工艺

薛叙明,吕春绪   

  1. 常州工程职业技术学院南京理工大学化工学院
  • 出版日期:2009-11-05 发布日期:2009-11-05

Process for synthesizing ozagrel

XUE Xuming,LÜ Chunxu   

  1. Changzhou Institute of Engineering TechnologyCollege of Chemical EngineeringNanjing University of Science & Technology
  • Online:2009-11-05 Published:2009-11-05

摘要: 研究了以4-甲基苯甲醛为原料,经克莱森缩合、N-溴代丁二酰亚胺(NBS)溴化、咪唑缩合以及碱条件下水解反应制得抗血栓药奥扎格雷的工艺。考察了反应物配比、温度控制、NBS用量、缩合反应碱的选择、水解碱用量控制等因素的影响,4步反应总收率为41.6%

Abstract: Ozagrelan anti-thrombosis drugwas synthesized from 4-methylbenzaldehyde by Claisen condensation with ethyl acetate to give ethyl 4-methyl cinnamatethen by bromination with NBS to give ethyl 4-bromomethyl cinnamatewhich was condensed with imidazole in alkaline followed by hydrolysis. The optimum process parameters were also determined with an overall yield of 41.6%.

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