【摘要】 <正>甘草次酸(glycyrrhetinic acid,2)是从豆科植物甘草的根茎中提取得到的五环三萜类化合物[1,2]。药理活性研究表明:2的3-羟基被取代后,其抗炎活性、抗溃疡活性较为显著,且3、30-位分别成酯后具有较高的抗炎活性[3]。本研究以乙酰甘氨酸和2为原料,在DCC／ DMAP体系[4]中合成了2的3位酯衍生物N-乙酰胺基乙酸甘草次酸酯(1),通过波谱分析确定其结构,合成路线见图1。并对18℃搅拌、40℃常规回流、40℃超声回流3种酯化条件采用HPLC法跟踪检测,确定了后法为合成1的最优方法。更多还原

【Abstract】 N-Acetyl glycine-glycyrrhetinic acid ester was synthesized by N-acetyl glycine and glycyrrhetinic acid in CH₂Cl₂ in the presence of DCC/DMAP under three different conditions respectively: stirring at 18℃, refluxing at 40℃, refluxing at 40℃ under ultrasonic radiation. The reaction speed of esterification was detected by HPLC. The results showed that the yield of ester was higher under the last condition in shorter reaction time.更多还原