A novel synthetic route for 2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethanamine

作者:Luo Xiao Chuan; Chen Guo Hua*; Bin Zhang Hui; Huang Wen Long
来源:Chinese Chemical Letters, 2008, 19(1): 59-60.
DOI:10.1016/j.cclet.2007.11.011

摘要

2-[2-(2,2,2-Trifluoroethoxy)phenoxy]ethanamine is the key intermediate of Silodosin, the alpha(1)-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.

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