| 尹贻虎,薛玉涛,窦春水,姚庆强.化学通报,2018,81(4):380-383. |
| 抗高压药马西替坦的合成及工艺优化 |
| Synthesis and Optimization of Antihypertensive agent Macitentan |
| 投稿时间：2018-01-03 修订日期：2018-01-29 |
| DOI： |
| 中文关键词: 马西替坦 合成 高血压 |
| 英文关键词:Macitentan, synthesis, hypertension |
| 基金项目: |
|
| 摘要点击次数: 3246 |
| 全文下载次数: 0 |
| 中文摘要: |
| 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六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，工艺操作更加简便，更有利于工业化生产。中间体和产物经1H-NMR和ESI-MS确证结构。 |
| 英文摘要: |
| 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. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
| 关闭 |
|
|
|