舒更葡糖钠的合成工艺

魏词; 王红

引用本文:	魏词,王红.舒更葡糖钠的合成工艺[J].中国现代应用药学,2016,33(4):431-433.
	WEI Ci,WANG Hong.Synthetic Process of Sugammadex Sodium[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(4):431-433.

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舒更葡糖钠的合成工艺
魏词¹, 王红²
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

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。

关键词: 合成工艺 γ-环糊精舒更葡糖钠

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Synthetic Process of Sugammadex Sodium

WEI Ci¹, WANG Hong²

1.Pharmacy of Maternal and Child Health Care Hospital of Hubei, Wuhan 430070, China;2.School of Pharmacy, Hubei University of Chinese Medicine, Wuhan 430065, China

Abstract:

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.

Key words: synthetic process γ-cyclodextrin sugammadex sodium