Chin. J. Org. Chem. ›› 2010, Vol. 30 ›› Issue (06): 898-903. Previous Articles     Next Articles




  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

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

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