| A novel synthetic route for 2-[2-（2,2,2-trifluoroethoxy）phenoxy]ethanamine |
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| 引用本文： | Xiao Chuan Luo Guo Hua Chen Hui Bin Zhang Wen Long Huang. A novel synthetic route for 2-[2-（2,2,2-trifluoroethoxy）phenoxy]ethanamine[J]. 中国化学快报, 2008, 19(1): 59-60. DOI: 10.1016/j.cclet.2007.11.011 |
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| 作者姓名： | Xiao Chuan Luo Guo Hua Chen Hui Bin Zhang Wen Long Huang |
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| 作者单位： | a Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;b Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China |
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| 摘 要： | 2-[2-（2,2,2-Trifluoroethoxy）phenoxy]ethanamine is the key intermediate of Silodosin, the α1-adrenoceptor antagonist for the treatment of benign prostatic hyperplasia. In order to obtain this intermediate, we developed a novel synthetic route by utilizing 2- nitrochlorobenzene as the starting material via O-alkylation, reduction, diazotization, acidolysis, etherification, condensation and hydrazinolysis. The highlight of this method lies on its convenience and economy in accessing this intermediate. 2007 Guo Hua Chert. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
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| 关 键 词： | 乙烷胺 合成 有机化学 中间体 |
| 收稿时间： | 2007-09-18 |
A novel synthetic route for 2-[2-(2,2,2-trifluoroethoxy)phenoxy] ethanamine |
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| Xiao Chuan Luo,Guo Hua Chen,Hui Bin Zhang,Wen Long Huang. A novel synthetic route for 2-[2-(2,2,2-trifluoroethoxy)phenoxy] ethanamine[J]. Chinese Chemical Letters, 2008, 19(1): 59-60. DOI: 10.1016/j.cclet.2007.11.011 |
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| Authors: | Xiao Chuan Luo Guo Hua Chen Hui Bin Zhang Wen Long Huang |
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| Affiliation: | a Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;b Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China |
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| Abstract: | 2-[2-(2,2,2-Trifluoroethoxy)phenoxy]ethanamine is the key intermediate of Silodosin, the α1-adrenoceptor antagonist for thetreatment of benign prostatic hyperplasia. In order to obtain this intermediate, we developed a novel synthetic route by utilizing 2-nitrochlorobenzene as the starting material via O-alkylation, reduction, diazotization, acidolysis, etherification, condensation andhydrazinolysis. The highlight of this method lies on its convenience and economy in accessing this intermediate. |
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| Keywords: | Silodosin 2-[2-(2,2,2-Trifluoroethoxy)phenoxy]ethanamine Synthesis |
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