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豆腐果苷-咪唑衍生物的合成及镇静活性研究
引用本文:吕世明,杨聪玲,赵辉,李颖,尹述凡.豆腐果苷-咪唑衍生物的合成及镇静活性研究[J].有机化学,2010,30(1):112-116.
作者姓名:吕世明  杨聪玲  赵辉  李颖  尹述凡
作者单位:四川大学化学学院,成都,610064
摘    要: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,~(13)C 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(400mg·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    镇静活性  合成
收稿时间:2009-04-04
修稿时间:2009-06-13

Synthesis and Calm Activity of Imidazole Derivatives of Helicid
LU Shiming,Yang Congling,Zhao Hui,Li Ying,Yin Shufan.Synthesis and Calm Activity of Imidazole Derivatives of Helicid[J].Chinese Journal of Organic Chemistry,2010,30(1):112-116.
Authors:LU Shiming  Yang Congling  Zhao Hui  Li Ying  Yin Shufan
Institution:(College of Chemistry,Sichuan University,Chengdu 610064)
Abstract: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,~(13)C NMR,IR and HRMS techniques.Their calm activities were investigated in healthy mice,and compound 4e showed favorable calm activity compared with helicid.
Keywords:helicid  imidazole derivative  2-hydroxy-1  2-diarylethanone  iodine  calm activity  synthesis
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