琥珀酸舒马曲坦的合成工艺改进

目的:改进琥珀酸舒马曲坦的合成工艺。方法:以4-肼基-N-甲基-苄基磺酰胺盐酸盐与4,4-二甲氧基-N,N-二甲基-丁胺为起始原料,改用多聚磷酸和磷酸二氢钠作为催化剂,后处理采用异丙醚和丙酮作为重结晶溶剂,经缩合、重排、环合、成盐的4步反应合成琥珀酸舒马曲坦。结果:获得纯度和收率均较满意的目标产物,总收率由文献报道的8.5%提高到12.7%。结论:此改进后的合成工艺成本低,操作简便易行,适于工业化生产。

An Improved Process for the Synthesis of Sumatriptan Succinate

Objective:To improve the process for the syntesis of sumatriptan succinate.Methods:The target compound was synthesized using 4-hydrazino-N-methyl-benzyl-sulphonamide hydrochloride and 4,4-dimethoxy-N,N-dimethyl butylamine as the starting materials,PPA and sodium dihydrogen phosphate instead as catalysts and isopropyl ether and acetone as solvents for recrylstallization,via 4-step reactions:condensation,rearrangement,cyclization and salt formtion.Results:The target compound was obtained with higher yield and purity.The total yield increased from literature-reported 8.5% to 12.7%.Conclusion:The improved process for the synthesis of sumatriptan succinate is of low cost,easy and suitable for the industrial manufacture.