Improved synthesis of raltegravir

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.}