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.
- 出版日期2008-1
- 单位中国药科大学