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Raltegravir的合成工艺研究(英文)

Improved synthesis of raltegravir

  • 摘要: 目的 : 研究治疗获得性免疫缺陷综合症药物raltegravir的合成工艺。 方法 : 经过成氨基腈,苄氧羰基保护氨基,从腈成氨肟,环合成二羟基嘧啶,氮甲基化,微波催化成酰胺,脱保护,再经酰化缩合成酰胺等8步反应制备raltegravir。 结果 : 经过对合成工艺的改进得到了目标产物,其结构经1H NMR,13C NMR,LR-MS和HR-MS确证,总收率为12.0%。 结论 :此方法原料易得、操作简单、成本低。

     

    Abstract: Aim :To develop a practical synthetic route of raltegravir,a drug for HIV treatment. Methods :Raltegravir was synthesized through an eight-step process including aminonitrile formation,protection with benzyloxycarbonyl group,conversion of the nitrile to the amidoxime,cyclization to form hydroxypyrimidinone,N-methylation,amidation with microwave-assistance,deprotection,amidation with acyl chloride. Results :The overall yield of the eight-step synthesis is about 12.0% and the structure of the target compound was confirmed by 1H NMR,13C NMR,LR-MS and HR-MS. Conclusion :The reported synthetic process of raltegravir highlights the advantages in terms of readily available starting materials,convenient operation and low cost.

     

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