摘要
为寻找高效低毒的三环类镇痛药物,以含氟-2-硝基甲苯为原料,经偶合、还原、缩合得到含氟二氢二苯并氮杂,再与3-氨基氯代丙烷进行N-烷基化反应,合成了12个未见文献报道的含氟丙米嗪类似物,讨论了关键中间体含氟二氢二苯并氮杂的合成条件,产物结构经1HNMR,IR,MS和元素分析确证.采用经典的小鼠热板法对所合成的化合物进行了镇痛活性的研究,活性测试结果表明6个新化合物的镇痛活性明显高于母体化合物丙米嗪.
In order to explore high efficacy and low toxicity analgetics,twelve novel imipramine analoges have been synthesized by the N-alkyl reaction of substituted 3-amino propyl chloride with fluoro-10,11-dihydro-5H-dibenz[b,f]-azepine,which was prepared by coupling,reduction and condensation from substituted 2-nitrotoluene.The reaction conditions of the key intermediate were discussed.Their structures were confirmed by ^1H NMR,IR,MS techniques and elemental analysis.The analgetic activity in vitro was evaluated by classic hot plate method in mice.The preliminary experimental results showed that the bioactivities of some derivations of imipramine were higher than that of the parent.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2010年第6期898-903,共6页
Chinese Journal of Organic Chemistry
基金
郑州大学引进人才基金(No.2005~2008)
河南省教育厅基金(No.2010A350005)资助项目
关键词
丙米嗪
丙米嗪类似物
合成
镇痛活性
imipramine
imipramine analoges
synthesis
analgetic activity
