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A novel synthetic route for 2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethanamine
Chinese Chemical Letters ( IF 9.4 ) Pub Date : 2008 , DOI: 10.1016/j.cclet.2007.11.011
Xiao Chuan Luo , Guo Hua Chen , Hui Bin Zhang , Wen Long Huang

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.

中文翻译:

2- [2-(2-(2,2,2-三氟乙氧基)苯氧基]乙胺的新颖合成途径

2- [2-(2,2,2-三氟乙氧基)苯氧基]乙胺为西洛多辛,所述α的关键中间体1 -肾上腺素能受体拮抗剂用于治疗良性前列腺增生的治疗。为了获得该中间体,我们通过以2-硝基氯苯为原料,通过O-烷基化,还原,重氮化,酸解,醚化,缩合和肼解,开发了一种新颖的合成路线。该方法的亮点在于使用该中间体的便利性和经济性。
更新日期:2017-01-31
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