磺达肝癸钠甲苷单糖中间体的合成工艺改进研究  

Improvement of method for synthesis of methyl glucosamine intermediate of fondaparinux sodium

作　　者：孙福亮[1] 韩健[1] 常淑梅[1] 侯文锋[1] 李振重 袁海新 干浩[1] 

机构地区：[1]天津红日药业股份有限公司,天津301700

出　　处：《现代药物与临床》2016年第3期269-272,共4页Drugs & Clinic

基　　金：天津市科技计划项目(13ZCZDSY00600)

摘　　要：目的对磺达肝癸钠中单糖中间体的合成工艺进行改进研究。方法以D-氨基葡萄糖为起始原料,经甲苷反应、苄基化反应得到单糖中间体。结果得到了α构型磺达肝癸钠甲苷单糖片段产物,HPLC检测质量分数可达98%以上,总收率为41.2%。结论磺达肝癸钠甲苷单糖中间体的合成工艺可简化操作,降低成本,提高安全性,方便生产。Objective To study the improved method for synthesis of methyl glucosamine intermediate of fondaparinux sodium. Methods D-Glucosamine was used as starting material to synthesize the target compound by methyl glycosylation and benzylation. Results The methyl α-glucosamine intermediate of fondaparinux sodium was synthesized. The purity reaches above 98% by HPLC, and the total yield was 41.2%. Conclusion The synthetic technology of methyl glucosamine intermediate of fondaparinux sodium can simplify the operation, reduce the cost, improve the safety, and is convenient for production.

关 键 词：磺达肝癸钠 甲苷反应 α、β异构体 

分 类 号：R914[医药卫生—药物化学]