一种改进的依替唑仑合成方法 |
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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. |
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作者姓名: | 开永茂 李 磊 赵廷兴 董 战 张丽娟 梁德辉 李鸿波 |
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作者单位: | 西南科技大学材料科学与工程学院,四川绵阳621010 |
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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). |
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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。
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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 |
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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) |
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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. |
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Keywords: | Etizolam 2 - Amino - 3 - (2 - chlorobenzoyl) - 5 - ethylthiophene Urotropin |
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