Citation: 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 shu

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

a Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;
b Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China

Received Date: 18 September 2007

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.
- Silodosin,
- 2-[2-(2,2,2-Trifluoroethoxy)phenoxy]ethanamine,
- Synthesis
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