伐地考昔的合成  

Synthesis of Valdecoxib

作　　者：黄远珺[1] 刘明星[1] 郭年春[1] 姚勃 

机构地区：[1]湖北工业大学生物工程学院,武汉430068 [2]武汉百科药物开发有限公司,武汉430056

出　　处：《中国现代应用药学》2009年第6期465-466,共2页Chinese Journal of Modern Applied Pharmacy

基　　金：湖北省科技攻关项目(2005AA301B01);湖北省教育厅青年基金(2004Q001)

摘　　要：目的合成伐地考昔并改进其工艺。方法以苯乙腈和苯甲酸甲酯为起始原料,经Claisen缩合一锅法得关键中间体苯基苄基甲酮,然后经羟胺化、环合和磺酰胺化等反应得戊地昔布。结果所得产物经IR、1H-NMR和MS确证了其结构,产物总产率约33.71%。结论此工艺方法简便,原料易得,便于工业化生产。OBJECTIVE To synthesize valdecoxib and optimize the process. MOTHODS The key intermediate of phenyl benzyl ketone was prepared by the one-pot method using Claisen condensation reaction with phenylacetonitrile and methyl benzoate as materials. Then valdecoxib was synthesized by a series reaction of hydroxylamine, cyclozation and sulfanilamide. RESULTS The structure of product was characterized by IR, ^1H-NMR and MS. The overall yield of valdecoxib was about 33.71%. CONCLUSION This process can be easily controlled and is suitable for a scale production.

关 键 词：伐地考昔 非甾体抗炎药 合成 

分 类 号：TQ460.6[化学工程—制药化工]