In order to find new a1-receptor inhibitors with high selectivity, seven 1-(3-benzoyl-1-phenoxyl)-3-(4-phenylpiperazin-1-yl)-propan-2-ol and 1-(4-methoxyphenoxy)-3-(4-arylpiperazin-1-yl)-propan-2-ol derivatives (5a-5g) were synthesized through substitution reaction of 3-chloro-1,2-epoxypropane (2) with 3-hydroxylbenzophenone or 4-methoxylphenol in alkaline condition, followed by the ring cleavage of 3-substituted phenoxy-1,2-epoxypropane (3) with arylpiperazine. All the target compounds were identified by their 1HNMR, MS, IR spectra and elemental analysis. The response of rat anococcygeus muscle to these compounds in vitro was tested, and the bioassay indicated that all the compounds had potent antagonistic activity against 1-receptor(pA2＞6), and compound (5g) showed the best potency（pA2=8.13±0.25）.