| 一种改进的依替唑仑合成方法 |
| |
| 引用本文： | 开永茂,李 磊,赵廷兴,董 战,张丽娟,梁德辉,李鸿波.一种改进的依替唑仑合成方法[J].西南科技大学学报,2014(1):10-12. |
| |
| 作者姓名： | 开永茂 李 磊 赵廷兴 董 战 张丽娟 梁德辉 李鸿波 |
| |
| 作者单位： | 西南科技大学材料科学与工程学院,四川绵阳621010 |
| |
| 基金项目： | 碳纳米材料四川省青年科技创新研究团队专项（2011JTD0017）. |
| |
| 摘 要： | 依替唑仑是-种在临床上应用较为广泛的镇静、催眠、抗抑郁药。以2-氨基-3-（2-氯苯甲酰）-5-乙基噻吩（I）为原料，经氯乙酰化，再在乙醇中与乌洛托品环合，制得关键中间体（Ⅲ）。中间体（Ⅲ）经硫化、环合反应制得依替唑仑（V），4步反应总收率为56．4％。改进后的反应具有合成路线短、条件温和、操作简便、收率高等优点。
|
| 关 键 词： | 依替唑仑2-氨基-3-（2-氯苯甲酰）-5-乙基噻吩乌洛托品 |
An Improved Synthesis of Etizolam |
| |
| Institution: | KAI Yong- mao, LI Lei, ZHAO Ting- xing, DONG Zhan, ZHANG Li -juan, LIANG De- hui, LI Hong- bo ( School of Materials Science and Engineering, Southwest University of Science and Technology, Mianyang 621010, Sichuan , China) |
| |
| Abstract: | Etizolam is a sedative, hypnotic and antidepressant drug widely used in clinics. In this study,the key intermediate （ m ） was synthesized through acetylation and then cyclization in ethanol with uro-tropin from 2 - amino - 3 - （ 2 - chlorobenzoyl） - 5 - ethyhhiophene （ I ） as raw material. The targetproduct etizolam （ V ） was successfully obtained from 111 via sulfuration and cyclization. The total yield ofthe four steps was 56.4%. The improved synthetic process has such advantages as short synthetic route,mild reaction condition, simple operation, high yield and so on. |
| |
| Keywords: | Etizolam 2 - Amino - 3 - （2 - chlorobenzoyl） - 5 - ethylthiophene Urotropin |
| 本文献已被 CNKI 维普 等数据库收录！ |
|
