5-[(2R)-[2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2-meth- oxybenzenesulfonamide, a pharmaceutical composition containing the compound, and the synthesis method thereof. The compound has strong antagonism toward .alpha.1-adrenceptor and has high selectivity toward smooth muscle of urethra. ##STR00001##