摘要
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。
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-dime- thoxy-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 fonntion. 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.
出处
《药学进展》
CAS
2007年第4期171-173,共3页
Progress in Pharmaceutical Sciences
关键词
琥珀酸舒马曲坦
合成
工艺
Sumatriptan succinate
Synthesis
Process
