| 瑞巴匹特羧乙酯的合成 |
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| 引用本文： | 张立娟,张珩,杨艺虹,周刚,郑雅婧,张秀兰.瑞巴匹特羧乙酯的合成[J].武汉化工学院学报,2009,31(3):23-25. |
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| 作者姓名： | 张立娟 张珩 杨艺虹 周刚 郑雅婧 张秀兰 |
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| 作者单位： | 武汉工程大学绿色化工过程省部共建教育部重点实验室,湖北武汉430074 |
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| 基金项目： | 湖北省科技厅项目（2004AA301C0）资助 |
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| 摘 要： | 以N-乙酰乙酰苯胺为原料，经溴化、环合制得4-溴甲基喹啉-2-酮（Ⅲ）；由盐酸氨基丙二酸二乙酯经酰化制得4-氯苯甲酰胺基丙二酸二乙酯（Ⅳ）；最后用4-溴甲基喹啉-2-酮（Ⅲ）和4-氯苯甲酰胺基丙二酸二乙酯（Ⅳ）经烃化反应合成瑞巴匹特羧乙酯（Ⅰ）．结果表明：在n（Ⅳ）：n（Ⅲ）：n（乙醇钠）=1：1：1．2，回流反应2h时，合成总收率63．81％（以N-乙酰乙酰苯胺计）．
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| 关 键 词： | 瑞巴匹特 中间体 瑞巴匹特羧乙酯 合成 |
Synthesis of diethyl ribamipide carboxylate |
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| ZHANG Li-juan,ZHANG Heng,YANG Yi-hong,ZHOU Gang,ZHENG Ya-jing,ZHANG Xiu-lan.Synthesis of diethyl ribamipide carboxylate[J].Journal of Wuhan Institute of Chemical Technology,2009,31(3):23-25. |
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| Authors: | ZHANG Li-juan ZHANG Heng YANG Yi-hong ZHOU Gang ZHENG Ya-jing ZHANG Xiu-lan |
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| Affiliation: | (Key Laboratory for Green Chemical Process of Ministry of Education, Wuhan Institute of Technology, Wuhan 430074,China) |
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| Abstract: | The diethyl-2-（ 4-chlorobenzoylamino ）-2-（ 1, 2-dihydro-2-oxo-4-quinolyl ） malonate, an intermediate of ribamipide was synthesized from N-Acetoacetanilide as material. Firstly, 4- （bromomethyl）-quinolin-2（1H）-one was obtained by the bromination and cyclization. Then, diethyl-2- （4-chlorobenzamido）malonate was obtained by the acylation of diethyl aminomalonate hydroehloride. Finally, diethyl-2-（4-chlorobenzoylamino）-2- （1,2-dihydro-2-oxo-4-quinoiyl） malonate was prepared by alkylation of 4-（ bromomethyl）-qui-nolin-2 （ 1H ）-one with diethyl-2-（4-chlorobenzamido） malonate, under the conditions which were as follows： the molar ratio of Ⅳ to Ⅲto sodium alcoholate was 1 ： 1：1.2 ,the refluxed time was 2 h. The total yield was 63.81% （with N-Acetoacetanilide as the material）. |
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| Keywords: | ribamipide intermediate 2-（ 4-chlorobenzoylamino ）-2-（ 1 2-dihydro-2-oxo-4-quinol-yl ） malonate synthesis |
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