【作者】 姜乃才； 孟庆国； 周莎莎； 马小涛；

【Author】 Jiang Nai-cai, Meng Qing-guo, Zhou Sha-sha, Ma Xiao-tao (School of Pharmacy, Yantai University, Yantai 264005)

【机构】 烟台大学药学院；

【摘要】 本研究工作设计合成了6个乌索酸(UA)衍生物(1-6)。UA钠盐与溴乙烷反应制得乌索酸乙酯(4),UA和化合物4与二元酸酐反应生成相应的乌索酸二元酸单酯,然后转化成相应的钠盐(1,2,5,6)。在吡啶介质中,UA与氧氯化磷发生酰化反应,产物水解得到化合物3。初步试验表明,与乌索酸及其钠盐相比,化合物(1,2,3,5和6)在水中的溶解度(25℃)均大于3 g／100 ml,其水溶性明显得到改善。化合物1～6均为乌索酸的前体药物,其中,化合物3、5、6目前尚未见文献报道。更多还原

【Abstract】 Six derivatives 1~6 of Ursolic acid (UA) have been designd and synthesized in this study. The ethyl ester of Ursolic acid (4) was prepared from sodium Ursolic acid with bromoethane. UA and compound 4 reacted with dibasic acid anhydrides to give the dibasic acid monoesters of Ursolic acid, which were subsequently transformed into their sodium salts (1, 2, 5, 6). UA was acylated by phosphorus oxychloride in pyridine to give the intermediate compound 3A, which was hydrolyzed and transformed into its sodium salt (3). In some preliminary experiments, it was shown that the solubilities in water of compounds 1, 2, 3, 5 and 6 are all over 3 g/100 ml at 25℃, which were much better improved compared to Ursolic acid or its sodium salt. The pro-drugs of Ursolic acid (3,5 and 6) have not been reported previously.更多还原