盐酸缬更昔洛韦的合成路线优化  

Optimization of Synthetic Route of Valganciclovir Hydrochloride

作　　者：汪小兵 尹先清[1] 许方亮 李俊 李立威[2] 

机构地区：[1]长江大学化学与环境工程学院,湖北荆州434023 [2]荆楚理工学院湖北省荆门医药工业技术研究院,湖北荆门448000

出　　处：《长江大学学报（自然科学版）》2018年第9期25-27,共3页Journal of Yangtze University(Natural Science Edition)

基　　金：湖北省高等学校优秀中青年科技创新团队计划项目(T200911)

摘　　要：设计了一条简便可行的盐酸缬更昔洛韦合成路线,路线以单乙酰更昔洛韦为起始原料,在羰基二咪唑和缚酸剂三乙胺的作用下和叔丁氧羰基保护的缬氨酸进行单酯化反应,然后再经过"一锅煮"分别脱去其侧链缬氨酸上的保护基和更昔洛韦的羟基上保护基得到目标产物,路线总收率为35.2%,目标产物纯度为98.9%,符合USP35标准规定。该方法具有路线短、操作简便、原料易得等优点,适于工业化生产。This paper designs a route of the synthesis of valganciclovir hydrochloride,the route start with monoacet ylganciclovir.It has a monesterification reaction with valine whose amino is protected by t-butyloxycarboryl,under the action of TEA,as acid binding agent,and CDI.And then,the protecting groups of hydroxyl and amino are removed to obtain the target product by one-pot procedure.The route has a total yield for 35.2%.This method has the advantages of short route,easy operation and readily available for raw materials,which is suitable for industrial production.

关 键 词：单乙酰更昔洛韦 叔丁氧羰基 一锅煮 合成 缬更昔洛韦 

分 类 号：TQ46[化学工程—制药化工]