舒更葡糖钠的合成工艺  

Synthetic Process of Sugammadex Sodium

作　　者：魏词 王红[2] 

机构地区：[1]湖北省妇幼保健院药剂科,武汉430070 [2]湖北中医药大学药学院,武汉430065

出　　处：《中国现代应用药学》2016年第4期431-433,共3页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的改进舒更葡糖钠的合成工艺。方法以γ-环糊精为原料,先用关键中间体(2)经过选择性溴代,然后再经成醚反应,合成舒更葡糖钠。结果目标化合物经1H-NMR和HRMS确证结构,反应总收率>30%。结论该合成路线成本低廉,操作简便,有良好的工业化生产前景。OBJECTIVE To optimize synthetic process of sugammadex sodium. METHODS Sugammadex sodium was synthesized from γ-cyclodextrin through selective bromination using the key immediate 2 and subsequent thioetherifation. RESULTS The goal product was structurally identified by 1H-NMR and HRMS, and the total yield was 〉30.0%. CONCLUSION This process has the advantages of low-cost, simple operation and good prospects for commercial scale-up.

关 键 词：合成工艺 Γ-环糊精 舒更葡糖钠 

分 类 号：R914.5[医药卫生—药物化学]