环磷酰胺酯的合成研究  

Study on synthesis of phosphoramidate compounds

作　　者：吕海燕[1] 王倩[1] 张南京 赵玉芬[1] 

机构地区：[1]清华大学化学系生命有机磷化学国家教委开放实验室

出　　处：《清华大学学报（自然科学版）》1997年第12期44-46,共3页Journal of Tsinghua University(Science and Technology)

基　　金：国家自然科学基金

摘　　要：环磷酰胺酯类化合物是一类对癌症疗效显著的化合物。其药效往往与其立体结构密切相关。文中采用新的合成方法，利用２，２，４－三甲基－１，３－戊二醇与三氯化磷反应得到环状二烷基亚磷酸酯，然后再利用此亚磷酸酯与一些胺类、氨基酸酯类化合物反应，合成了一系列未见报道的含磷杂环环磷酰胺酯类化合物，并利用红外、核磁、质谱等分析手段对其结构进行了鉴定。结果表明，该方法具有较高的立体选择性，且实验条件温和，操作简单，中间产物环状二烷基亚磷酸酯不用分离纯化，是一种较为理想的合成反式环磷酰胺酯的方法。产物的生物活性正在测试中。Cyclic phosphoramidate compounds are widely used as a type of anticancer medicines and their stereo structures are directly related to their activities and effects. A series of cyclic phosphoramidates——Nsubstituted 5,5dimethyl4(1methylethyl)1,3,2dioxaphosphorinane2 oxide, were synthesized conveniently by the reactions of cyclic phosphite Ⅵ with amino compounds. The results showed that the reactions were high stereospecific and nearly all the produced cyclic phosphoramidates were transisomers. The usefulness of this methodology also lies in the fact that the reactions were proceeded under mild conditions and the intermediatecyclic phosphite Ⅵ need not be separated and purified.

关 键 词：环磷酰胺酯 合成 抗癌药物 生物活性 

分 类 号：TQ463.3[化学工程—制药化工] O624.6[理学—有机化学]