含α-氨基膦酸酯齐墩果酸衍生物的合成

摘要

[ Objective ] The aim was to seek diverse lead compounds, the novel oleanolic acid derivatives containing α-a minophosphate moiety were designed and synthesized. [Methods] The group α-a mino acid aromatic esters and 3- oxo-oleanolic acid were spliced by the DCC/HOBt condensation reactions in DMK/DCM mixed medium. [Results] The four high water-soluble a-a minophosphonate oleanolic acid derivatives were synthesized with the protocol of mild reaction conditions,less by-products,raw materials readily available. [Conclusion] HOBt and DCC co-condensation was a highly efficient and practical approach for preparation of novel a-a minophosphonate oleanolic acid derivatives.%[目的]研究新型α-氨基膦酸酯齐墩果酸衍生物的合成方法.[方法]以DMF/DCM混合溶剂为反应介质,在DCC/HOBt作用下,经缩合反应将3-氧代修饰的齐墩果酸拼接上α-氧基膦酸芳香酯.[结果]合成了4个水溶性好、结构新颖的α-氨基膦酸酯齐墩果酸衍生物.[结论] HOBt与DCC协同缩合制备新型的α-氨基膦酸酯齐墩果酸衍生物是一种高效实用的方法.