N取代苄基氟哌啶醇氯化物及其还原物的合成与扩张血管活性
合成,,N取代苄基氟哌啶醇氯化物；合成；扩血管活性；构效关系,1材料与方法,2结果与讨论,3结论,参考文献
摘 要 目的 合成N取代苄基氟哌啶醇氯化物及其还原物并研究它们的扩张血管活性。 方法 以氟哌啶醇为原料，通过与取代氯苄化合物在回流下反应得到N取代苄基氟哌啶醇氯化物；用氢化硼钠将氟哌啶醇还原为氢化氟哌啶醇，再与取代氯苄化合物在回流下反应得到N取代苄基氢化氟哌啶醇氯化物；以兔胸主动脉螺旋条生物测定法研究其抑制血管收缩的活性。结果 合成了6个N取代苄基氟哌啶醇氯化物F8-13和5个N取代苄基氢化氟哌啶醇氯化物FB8-11，FB13；初步生物活性实验结果表明，F8-13表现出不同程度的拮抗KCl所致兔胸主动脉螺旋条收缩血管活性，其中化合物F11的血管收缩抑制活性最强；但FB8-11，FB13的活性均较低。结论 化合物F11扩张血管活性强于先导化合物，初步构效关系表明，N取代苄基氟哌啶醇氯化物中苄基苯环上取代基的电性和取代位置可能为影响扩血管活性的重要因素。关键词 N取代苄基氟哌啶醇氯化物；合成；扩血管活性；构效关系
Synthesis of Nsubstituted benzyl haloperidol chlorides and their vasodilating activities
ZHENG Jinhong, WANG Jinzhi, PAN Ying,SHI Ganggang
( 1.Department of Chemistry, Shantou University Medical School,Shantou,Guangdong 515041;2.Department of Pharmacology, Shantou University Medical School,Shantou,Guangdong 515041)
Abstract Objective To study the synthesis of Nsubstituted benzyl haloperidol chlorides, Nsubstituted benzyl hydrohaloperidol chlorides and their vasodilating activities. Methods Haloperidol was reacted with different substituted benzyl chloride in reflux condition to synthesize the title compounds F8-13. Haloperidol was reacted with sodium borohydride to form hydrohaloperidol, then reacted with different substituted benzyl chloride in reflux condition to synthesize the FB8-11 ......
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