| 莫吉司坦的合成 |
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| 引用本文： | 赵蕊,李玲,丁一,罗振福,孙有光. 莫吉司坦的合成[J]. 中国医药工业杂志, 2011, 42(1) |
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| 作者姓名： | 赵蕊 李玲 丁一 罗振福 孙有光 |
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| 作者单位： | 1. 天津理工大学化学化工学院,天津,300191
2. 天津药物研究院化学制药部,天津,300193 |
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| 摘 要： | 愈创木酚与2-溴代乙醛缩二甲醇发生亲核取代,再与半胱胺盐酸盐缩合闭环得到2-[(2-甲氧基苯氧基)甲基]噻唑烷,最后与氯甲酰乙酸乙酯反应得到外周非麻醉性镇咳药莫吉司坦,总收率约71%.
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| 关 键 词： | 莫吉司坦 外周非麻醉性镇咳药 合成 |
Synthesis of Moguisteine |
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| ZHAO Rui,LI Ling,DING Yi,LUO Zhenfu,SUN Youguang. Synthesis of Moguisteine[J]. , 2011, 42(1) |
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| Authors: | ZHAO Rui LI Ling DING Yi LUO Zhenfu SUN Youguang |
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| Affiliation: | ZHAO Rui~1,LI Ling~(2*),DING Yi~2,LUO Zhenfu~2,SUN Youguang~1 (1.Dept.of Chemistry and Chemical Engineering,Tianjin University of Technology,Tianjin 300191,2.Centre for Chemical Pharmaceutical Research,Tianjin Institute of Pharmaceutical Research,Tianjin 300193) |
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| Abstract: | Moguisteine,a novel peripheral non-narcotic antitussive drug,was synthesized from guaiacol by nucleophilic substitution with 2-bromoacetaldehyde dimethyl acetal and cyclization with cysteamine hydrochloride to give 2-[(2-methoxyphenoxy) methyl]thiazolidine,which was subjected to N-acylation with ethyl chloroformyl acetate. The overall yield was about 71%with purity of 99%. |
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| Keywords: | moguisteine peripheral non-narcotic antitussive drug synthesis |
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