| 苹果酸阿莫曲坦的合成 |
| |
| 引用本文： | 于圆圆,金华,李建其. 苹果酸阿莫曲坦的合成[J]. 中国医药工业杂志, 2011, 42(6) |
| |
| 作者姓名： | 于圆圆 金华 李建其 |
| |
| 作者单位： | 中国医药工业研究总院上海医药工业研究院,上海,200437 |
| |
| 基金项目： | 国家"重大新药创制"科技重大专项 |
| |
| 摘 要： | 对硝基氯苄经亚硫酸钠磺化、五氯化磷氯代、四氢吡咯取代、催化氢化、重氮化和还原制得4-(吡咯烷-1-基磺酰甲基)苯肼盐酸盐(7),与4-氯-1-羟基丁烷磺酸钠反应后,再经成腙、环合和甲基化"一锅法"制得阿莫曲坦粗品,经成富马酸盐纯化,再与苹果酸成盐制得苹果酸阿莫曲坦,总收率约6%(以对硝基氯苄计).
|
| 关 键 词： | 苹果酸阿莫曲坦 5-HT1B/1D受体激动剂 抗偏头痛药 合成 |
Synthesis of Almotriptan Malate |
| |
| YU Yuanyuan,JIN Hua,LI Jianqi. Synthesis of Almotriptan Malate[J]. , 2011, 42(6) |
| |
| Authors: | YU Yuanyuan JIN Hua LI Jianqi |
| |
| Affiliation: | YU Yuanyuan,JIN Hua,LI Jianqi(Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 200437) |
| |
| Abstract: | 4-(Pyrrolidine-1-sulfonylmethyl)phenylhydrazine hydrochloride(7) was synthesized from 4-nitrobenzyl chloride(2) by sulfonation with sodium sulfite,chlorination with phosphorus pentachloride,replacement with pyrrolidine,catalytic hydrogenation,followed by diazotization and reduction.Compound 7 was allowed to react with sodium 4-chloro-1-hydroxybutane-1-sulfonate,and then by hydrazone formation,cyclization and methylation to give almotriptan,which was purified by formation of its fumarate and reacted with mal... |
| |
| Keywords: | almotriptan malate 5-HT1B/1D receptor agonist antimigraine synthesis |
| 本文献已被 CNKI 万方数据 等数据库收录！ |
|
