联苯取代哌嗪丙醇类α_1受体阻滞剂的合成

Synthesis of 1-Phenoxy-3-[(4-biphenyl)piperazin-1-yl] propan-2-ol as α_1- Receptor Antagonist

芳基哌嗪类化合物是一类具有α1受体亚型选择性的α1受体阻滞剂。文章采用苯酚与3-氯-1,2-环氧丙烷反应得到苯氧基取代环氧丙烷,再用联苯取代哌嗪对环氧开环,合成了联苯取代哌嗪-2-丙醇类衍生物,总收率达64%以上。合成的目标化合物均经MS和1H-NMR谱进行了结构确认。

Arylpiperazine derivatives are a group of α1 receptor antagonists with subtype selectivity of α1-adrenoceptor. 3-[（4-biphenyl）piperazin-1-y1] propan-2-ol derivatives were synthesized by the reaction of phenol and 3-chloro-1,2-epoxypropane, followed by the ring cleavage of 3-phenoxy-1,2-epoxypropane with biphenylpiperazin. The total yield of objective compounds was above 64 %, and the structures of target compounds were confirmed by MS, 1H-NMR data.