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。

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.