有机化学 ›› 2010, Vol. 30 ›› Issue (01): 112-116. 上一篇    下一篇

研究简报

豆腐果苷-咪唑衍生物的合成及镇静活性研究

吕世明,杨聪玲,赵 辉,李 颖,尹述凡*   

  1. (四川大学化学学院 成都 610064)
  • 收稿日期:2009-04-04 修回日期:2009-06-13 发布日期:2010-01-20
  • 通讯作者: 尹述凡 E-mail:chuandayouji217@163.com

Synthesis and Calm Activity of Imidazole Derivatives of Helicid

Lü,Shiming,Yang,Congling,Zhao,Hui,Li,Ying,Yin,Shufan*   

  1. (College of Chemistry,Sichuan University,Chengdu 610064)
  • Received:2009-04-04 Revised:2009-06-13 Published:2010-01-20

以豆腐果苷、2-羟基-1,2-二芳基乙酮(2a~2d)、乙酸铵和脂肪胺为原料,碘单质作为催化剂,成功地合成了一系列豆腐果苷-咪唑类衍生物4a~4h,新化合物4a~4h的结构经1H NMR,13C NMR,IR和HRMS确认。并用小白鼠实验对目标化合物4a~4h进行了镇静活性筛选,其中4e (400 mg•kg-1)与豆腐果苷相比有较强的镇静活性。

关键词: 豆腐果苷, 咪唑衍生物, 2-羟基-1,2-二芳基乙酮, 碘, 镇静活性, 合成

A convenient approach for synthesis of the imidazole derivatives of helicid 4a~4h is presented via condensation of helicid,2-hydroxy-1,2-diarylethanone (2a~2d),ammonium acetate and alkyl amine,using iodine as efficient catalyst。The structures of the target compounds 4a~4h were characterized by 1H NMR,13C NMR,IR and HRMS techniques。Their calm activities were investigated in healthy mice,and compound 4e showed favorable calm activity compared with helicid.

Key words: helicid, imidazole derivative, 2-hydroxy-1,2-diarylethanone, iodine, calm activity, synthesis