齐多夫定合成工艺的改进

An Improved Synthesis Process of Zidovudine

齐多夫定是重要的抗艾滋病毒药物,也是目前抗艾滋病药物中最基本的组合成分。现有合成方法存在原料来源及成本等问题,研究及改进其合成工艺具有重要的经济效益和社会效益。本文以β胸苷为起始原料,经三苯基氯甲烷,甲磺酰氯保护,碱性条件下成环,叠氮化,脱保护等工艺制备齐多夫定。采用的反应条件温和,总收率达64.9%;本文方法简便、经济环保,对工业化生产有重要的指导意义。

Zidovudine （AZT） is an important drug prescribed alone or in combination with other drugs for the treatment of the human immunodeficiency virus infection（H IV）. Therefore, to study and improve the synthesis of AZT has great economic and social benefits. The synthesis of AZT has some obvious disadvantages in practice, for instance, the availability and cost of materials. Starting with 13-thymidylic, this route included the protection of hydroxyl group with triphenylchloromethane and methanesulfonyl chloride, the cyelization under alkaline condition, azidilization, and deprotection. The reaction condition was mild and the total yield was up to 64. 9%. The synthetic route is simple, economic and suitable for industrialization.