舒马曲坦的合成

Synthesis of sumatriptan

目的合成抗偏头痛药舒马曲坦。方法以对硝基氯苄为起始原料,经取代、胺化、还原、重氮化、环合等10步反应得到目标化合物舒马曲坦,总收率为18%。结果与结论目标化合物的结构经1H-NMR、IR和MS确证。该合成方法,反应条件温和,操作简便,原料易得,适合工业化生产。

Aim To investigate the synthetic method of sumatriptan as an anti-migraine agent. Methods Starting from p-nitrobenzylchloride, the target compound was synthesized through a ten-step procedure including substitution, amination, reduction, diazotization, cyclization and so on, and the overall yield was 18 %. Results and conclusion The structure of sumatriptan was characterized by ^1H-NMR, IR and MS. The procedure developed has several advantages such as mild reaction condition, convenient operation and easily obtained material. The synthetic method is suitable for industrial manufacture.