伐地考昔的合成

    Synthesis of Valdecoxib

    • 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.

       

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