| 盐酸普拉克索的合成 |
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| 引用本文： | 汪文婷,宁剑波,王凌云,李振华.盐酸普拉克索的合成[J].中国医药工业杂志,2012(7):524-526. |
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| 作者姓名： | 汪文婷 宁剑波 王凌云 李振华 |
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| 作者单位： | 1. 浙江工业大学药学院,浙江杭州,310014
2. 浙江台州清泉医药化工有限公司,浙江仙居,317300 |
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| 摘 要： | 4-乙酰胺基环己醇或4-苯甲酰胺基环己醇经TEMPO/NaOC1/NaBr体系氧化制得相应的酮,经溴代、环合、水解"一锅法"制得2,6-二氨基-4,5,6,7-四氢苯并噻唑(6),再经L-(+)-酒石酸拆分、丙烷基化及成盐制得抗帕金森病药盐酸普拉克索,总收率为9%。
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| 关 键 词： | 普拉克索 抗帕金森病药 合成 |
Synthesis of Pramipexole Dihydrochloride |
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| Authors: | WANG Wenting NING Jianbo WANG Lingyun LI Zhenhua |
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| Institution: | 1) (1.College of Pharmaceutical Sciences,Zhejiang University of Technology,Hangzhou 310014; 2.Zhejiang Taizhou Spring Pharmaceutical and Chemical Industry Company,Xianju 317300) |
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| Abstract: | 4-(N-Acetylamino) cyclohexanol or N-(4-hydroxycyclohexyl)benzamide were oxidized with TEMPO/NaOCl/NaBr to give corresponding ketones,which was subjected to bromination,cyclization and hydrolysis in one pot to give 2,6-diamino-4,5,6,7-tetrahydrobenzothiazole(6),then resolution with L-(+) -tartaric acid,propylation and salification to give pramipexole dihydrochloride in 9%overall yield. |
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| Keywords: | pramipexole antiparkinsonian agent synthesis |
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