| 佐米曲坦的合成研究 |
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| 引用本文： | 李金鹏,顾君琳,王晓琴,杨琍苹. 佐米曲坦的合成研究[J]. 华东师范大学学报(自然科学版), 2002, 0(3): 61-65 |
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| 作者姓名： | 李金鹏 顾君琳 王晓琴 杨琍苹 |
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| 作者单位： | 华东师范大学,化学系,上海,200062 |
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| 摘 要： | 佐米曲坦是一种具有很强选择性的5－HT1B／1D受体激动剂，用于治疗偏头痛，已在英国等上市，市场前景看好。该文研究了一条部分用一釜法的全成路线，以（L）－苯丙氨酸为原料，经硝化、酯化、酰胺化、还原（硝基）、还原（酯）、环化、重氮化、还原（重氮盐）和费歇尔吲哚合成共九步反应得到佐米曲坦，总产率为8.1%。作者改进了硝化反应的生产工艺，将酯化反应的产率由76％提高到92％，并尝试了新的（S）－4－（4－胺基苄基）－2－恶唑烷酮合成方法。
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| 关 键 词： | 偏头痛 佐米曲坦 合成 硝化反应 酯化反应 生产工艺 5－HT1B／1D受体激动剂 |
| 文章编号： | 1000-5641(2002)03-0061-05 |
| 修稿时间： | 2001-09-01 |
The Synthesis of Zolmitriptan : A Drug for Antimigraine |
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| LI Jin peng,GU Jun lin,WANG Xiao qin,YANG Li ping. The Synthesis of Zolmitriptan : A Drug for Antimigraine[J]. Journal of East China Normal University(Natural Science), 2002, 0(3): 61-65 |
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| Authors: | LI Jin peng GU Jun lin WANG Xiao qin YANG Li ping |
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| Abstract: | Zolmitriptan, a sort of selective 5-HT 1B/1D -like receptor agonist, is used in the treatment of migraine. Now it has been launched in Great British, and the market prospect is very good. In this essay, we have studied a one-pan synthesis routine of zolmitriptan. Zolmitriptan was synthesized from L pheneylalanine via nitration, esterification, amidation, reduction ( NO 2 ), reduction(-COOR), cylization, diazoium, reduction and Fischer indole synthesis in 8.1% overall yield. We have made progress in methodology of nitration reaction, and the yield of cylization step can be improved from 76% to 91.8%, and we tried a new synthetic method of (s)-4-(4-Aminobenzyl)-1,3-oxazolidin-2-one. |
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| Keywords: | migraine zolmitriptan synthesis |
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