| 米拉贝隆中间体2-氨基噻唑-4-乙酸的合成 |
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| 引用本文： | 黄婷,徐啸波,张纯宝,张华华.米拉贝隆中间体2-氨基噻唑-4-乙酸的合成[J].合成化学,2017,25(5):437-439. |
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| 作者姓名： | 黄婷 徐啸波 张纯宝 张华华 |
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| 作者单位： | 1. 大连理工大学(盘锦) 石油与化学工程学院，辽宁 盘锦 124221; 2. 衢州爱美康生物科技有限公司，浙江 衢州 324000 |
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| 基金项目： | 辽宁省科技攻关项目，大连理工大学大学生创新实验项目 |
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| 摘 要： | 以氰胺、硫和氯乙酰乙酸乙酯为原料，一水合对甲苯磺酸（TsOH·H2O）为催化剂，经成环反应制得2-氨基噻唑-4-乙酸乙酯（2); 2经水解反应合成了米拉贝隆中间体2-氨基噻唑-4-乙酸，其结构经1H NMR, 13C NMR, IR和元素分析确证。在最佳反应条件［1 0.25 mol, TsOH·H2O 0.01 mol,反应温度为80 ℃，重结晶溶剂（乙醇/水=1/1, V/V）］下，2收率88.2%。
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| 关 键 词： | 氯乙酰乙酸乙酯 2-氨基噻唑-4-乙酸 米拉贝隆 中间体合成 |
| 收稿时间： | 2016-10-31 |
Synthesis of The Intermediate for Mirabegron Aminothiazole-4-2-ethyl Acetic Acid |
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| HUANG Ting,XU Xiao-bo,ZHANG Chun-bao,ZHANG Hua-hua.Synthesis of The Intermediate for Mirabegron Aminothiazole-4-2-ethyl Acetic Acid[J].Chinese Journal of Synthetic Chemistry,2017,25(5):437-439. |
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| Authors: | HUANG Ting XU Xiao-bo ZHANG Chun-bao ZHANG Hua-hua |
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| Abstract: | Amino thiazole-4-2-ethyl acetate(2) was obtained by cyclization reaction, using cyanamide, elemental sulfur and chlorine ethyl acetoacetate as the starting materials, and TsOH·H2O as the catalyst.The intermediate for Mirabegron, aminothiazole-4-2-acetic acid, was synthesized by hydrolysis reaction of 2.The structure was confirmed by 1H NMR, 13C NMR, IR and elemental analysis.The yield of 2 was 88.2% under the optimum reaction conditions1 0.25 mol, TsOH·H2O 0.01 mol, reaction at 80 ℃, the recrystallization solvent was (EtOH/H2O=1/1, V/V)]. |
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| Keywords: | chlorine ethyl acetoacetate amino thiazole-4-2-ethyl acetic acid Mirabegron intermediate synthesis |
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