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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rahegravir.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,~(13)C 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.“,”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 benzyloxy-carbonyl group, conversion of the nitrile to the amidoxime, cyclization to form hydroxypyrimidinone, N-methyla-tion, 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, ~(13)C 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.