| 引用本文: | 黄远珺1，刘明星1*，郭年春1, 姚勃2.伐地考昔的合成[J].中国现代应用药学,2009,(6):465-466. |
| HUANG Yuanjun1, LIU Mingxing1*,GUO Nianchun1,YAO Bo2.Synthesis of Valdecoxib[J].Chin J Mod Appl Pharm(中国现代应用药学),2009,(6):465-466. |
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| 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。 |
| 关键词: 伐地考昔 非甾体抗炎药 合成 |
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| Synthesis of Valdecoxib |
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HUANG Yuanjun1, LIU Mingxing1*,GUO Nianchun1,YAO Bo2
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| 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. |
| Key words: valdecoxib nonsteoroidal anti-inflammatory drugs synthesis |
