舒更葡糖钠的合成工艺

Synthetic Process of Sugammadex Sodium

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.