| 抗高压药马西替坦的合成及工艺优化 |
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| 引用本文： | 尹贻虎,薛玉涛,窦春水,姚庆强.抗高压药马西替坦的合成及工艺优化[J].化学通报,2018,81(4):380-383. |
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| 作者姓名： | 尹贻虎 薛玉涛 窦春水 姚庆强 |
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| 作者单位： | 1.济南大学 山东省医学科学院医学与生命科学学院,1.济南大学 山东省医学科学院医学与生命科学学院,1.济南大学 山东省医学科学院医学与生命科学学院,1.济南大学 山东省医学科学院医学与生命科学学院 |
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| 摘 要： | 以4-溴苯乙酸甲酯为起始原料,经碳负离子亲核取代、关环、氯代、氮负离子亲核取代、氧负离子亲核取代等6步反应制得抗高血压药马西替坦,并对合成工艺进行了优化。优化后的工艺使中间体的纯度得到了提高,操作更加简便,更有利于工业化生产。中间体和产物的结构均经~1H-NMR和ESI-MS确证。
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| 关 键 词： | 马西替坦 合成 高血压 |
| 收稿时间： | 2018/1/3 0:00:00 |
| 修稿时间： | 2018/1/29 0:00:00 |
Synthesis and Optimization of Antihypertensive agent Macitentan |
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| YIN Yihu,XUE Yutao,DOU Chunshui and YAO Qingqiang.Synthesis and Optimization of Antihypertensive agent Macitentan[J].Chemistry,2018,81(4):380-383. |
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| Authors: | YIN Yihu XUE Yutao DOU Chunshui and YAO Qingqiang |
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| Institution: | School of Medicine and Life Sciences,University of Jinan-Shandong Academy of Medical Sciences,School of Medicine and Life Sciences,University of Jinan-Shandong Academy of Medical Sciences,School of Medicine and Life Sciences,University of Jinan-Shandong Academy of Medical Sciences,School of Medicine and Life Sciences,University of Jinan-Shandong Academy of Medical Sciences |
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| Abstract: | Using 4-bromophenylacetic acid methyl ester as the starting material, Macitentan was synthesized by a 6-step reaction of nucleophilic substitution of carbon anion, ring-closing reaction, chlorination, nucleophilic substitution of nitrogen anion, nucleophilic substitution of oxygen anion and the synthetic process was also optimized in this article. The improved process enhanced the purity of the intermediate, the operation was more convenient and it can be suitable for industrial production. The structures of the intermediates and products were confirmed by 1H-NMR and ESI-MS. |
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| Keywords: | Macitentan synthesis hypertension |
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