| 依托度酸的合成工艺 |
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| 引用本文： | 戴立言,王晓钟,陈英奇.依托度酸的合成工艺[J].化工学报,2005,56(8):1536-1540. |
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| 作者姓名： | 戴立言 王晓钟 陈英奇 |
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| 作者单位： | 浙江大学材料与化工学院制药工程研究所，浙江 杭州 310027 |
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| 摘 要： | 对非甾体抗炎药依托度酸的合成工艺进行了研究，以生产氯霉素原料对硝基乙苯时产生的大量副产物邻硝基乙苯为原料，先还原得邻乙基苯胺，然后经重氮化、亚硫酸钠还原得邻乙基苯肼盐酸盐，再与2,3-二氢呋喃反应得7-乙基色醇，不经分离，直接与3-氧代戊酸甲酯缩合成环、水解制得标题化合物.各步反应的最佳反应条件(反应温度，反应时间，摩尔收率)分别为，硝基还原：回流，3 h，96.2%;重氮化：0 ℃，0.5 h;重氮盐还原：70～75 ℃，3 h，(两步收率)92.5%;合成7-乙基色醇：回流，3 h;制备依托度酸甲酯：0 ℃，1.5 h，(两步)63.0%;酯水解：回流，2.5 h，95.0%.所得依托度酸甲酯和依托度酸物性与文献报道一致.
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| 关 键 词： | 依托度酸 药物合成 非甾体抗炎药 |
| 文章编号： | 0438-1157（2005）08-1536-05 |
| 收稿时间： | 06 28 2004 12:00AM |
| 修稿时间： | 2004-06-282004-08-16 |
Synthesis of etodolac |
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| DAI Liyan,WANG Xiaozhong,CHEN Yingqi.Synthesis of etodolac[J].Journal of Chemical Industry and Engineering(China),2005,56(8):1536-1540. |
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| Authors: | DAI Liyan WANG Xiaozhong CHEN Yingqi |
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| Abstract: | Synthesis of etodolac,a non-steroidal anti-inflammatory agent, was studied.In the study o-nitroethylbenzene as raw material was reduced by Fe / hydrochloric acid.The intermediate o-ethylaniline could be diazotized and reduced by sodium sulfite to give o-ethylphenylhydrazine,and 7-ethyltryptophol was obtained by condensation of o-ethylphenylhydrazine and 2,3-dihydrofuran in isobutanol as solvent.Finally 7-ethyltryptophol without separation reacted with methyl 3-oxopentanoate and was hydrolyzed to give the title compound.The optimal reaction conditions(temperature, time,molar yield) were as follows.Reduction of nitro group：reflux，3 h，96.2%;diazotization：0 ℃，0.5 h;reduction of diazonium salt：70—75 ℃，3 h，92.5%(two steps);synthesis of 7-ethyltryptophol：reflux，3 h;preparation of etodolac methyl ester：0 ℃，1.5 h，63.0%(two steps);hydrolysis：reflux，2.5 h，95.0%.The structures of etodolac and its methyl ester were the same as those reported in literature. |
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| Keywords: | etodolac pharmaceutical synthesis non-steroidal anti-inflammatory drug |
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