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

作　　者：季红[1] 欧阳菁[1] 袁牧[1] 

机构地区：[1]广州医科大学药学院,广东广州510182

出　　处：《广东化工》2013年第18期8-8,2,共2页Guangdong Chemical Industry

基　　金：广东省医学科研项目(B2010140);广州市珠江科技新星专项(2011J2200011);广州市教育局科研项目(10A257)

摘　　要：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.

关 键 词：苯氧基取代环氧丙烷 联苯取代哌嗪-2-丙醇类衍生物 合成 Α1受体阻滞剂 

分 类 号：R914[医药卫生—药物化学]