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

作　　者：Xiao Chuan Luo Guo Hua Chen Hui Bin Zhang Wen Long Huang 

机构地区：[1]epartment of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China [2]Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China

出　　处：《Chinese Chemical Letters》2008年第1期59-60,共2页中国化学快报（英文版）

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.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.

关 键 词：SILODOSIN 2-[2-（2 2 2-Trifluoroethoxy）phe＇noxy]ethanamine SYNTHESIS 

分 类 号：O621.3[理学—有机化学]