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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (06): 898-903. 上一篇    下一篇

研究简报

丙米嗪类似物的合成及其镇痛活性研究

李雯*,1，肖博2，周游3，刘宏民3   

  1. 1郑州大学化工与能源学院 郑州 450001)
    (2郑州轻工业学院河南省表界面科学重点实验室 郑州 450002)
    (3郑州大学药学院 郑州 450001
  • 收稿日期:2009-08-24 修回日期:2009-12-25 发布日期:2010-01-07
  • 通讯作者: 李雯 E-mail:liwenzzu@gmail.com

Synthesis and Analgetic Activity of Imipramine Analoges

Li Wen*,1 Xiao Bo2 Zhou You3 Liu Hongmin3   

  1. 1 College of Chemical and Energy Engineering, Zhengzhou University, Zhengzhou 450001)
    (2 Henan Provincial Key Laboratory of Surface & Interface Science, Zhengzhou University of Light Industry, Zhengzhou 450002)
    (3 Department of Medicinal Chemistry, Zhengzhou University, Zhengzhou 450001
  • Received:2009-08-24 Revised:2009-12-25 Published:2010-01-07
  • Contact: wen li E-mail:liwenzzu@gmail.com

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被引次数

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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1H NMR, 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.

关键词: 丙米嗪, 丙米嗪类似物, 合成, 镇痛活性

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.

Key words: imipramine, imipramine analoges, synthesis, analgetic activity