伐地考昔的合成

Synthesis of Valdecoxib

关键词:  伐地考昔  非甾体抗炎药  合成

Key words:  valdecoxib  nonsteoroidal anti-inflammatory drugs  synthesis

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。

Abstract:

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.