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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。
Cyclophosphamide esters are a class of compounds that have a significant effect on cancer. Its efficacy is often closely related to its three-dimensional structure. In this paper, a new synthesis method, the use of 2,2,4-trimethyl-1,3-pentanediol and phosphorus trichloride reaction of cyclic dialkyl phosphites, and then use this phosphite with some Amines and amino acid esters. A series of unreported phosphorus-containing heterocyclic cyclophosphamide esters were synthesized and their structures were identified by means of IR, NMR and MS. The results show that this method has a high stereoselectivity, and the experimental conditions are mild, easy to operate, the intermediate product of the dialkyl dialkyl phosphonates without separation and purification, is an ideal method for the synthesis of trans-cyclophosphamide ester . The biological activity of the product is being tested.