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
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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
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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 |