从Ｌ－丝氨酸出发，经酯化、环磷酰化、磷酰化、加硫等步骤得到替加氟、尿苷硫代环磷酰胺酯缀合物２、３．Ｌ－丝氨酸酯经Ｎ－烷基化，然后再与磷酰二氯关环，进一步与替加氟乙醇反应得到环磷脂缀合物４．考察了两种环磷酰化反应中碳手性中心对磷原子的不对称诱导效果，并用硅胶柱层析分离了产物２、３、４ 的非对映异构体．基于ＮＭＲ数据，对它们的构型进行了讨论和初步的确定，它们的抗癌活性正在测试当中． From L-serine, esterification, cyclophosphorylation, phosphorylation, sulfurization and other steps to obtain tegafur, uridine thiophosphamide ester conjugates 2,3. The L-serine ester is N-alkylated and then cyclized with phosphorus oxychloride to further react with tegafurhanol to give the cyclic phospholipid conjugate 4. The asymmetric induction of phosphorus atoms by carbon chiral centers in two cyclophosphorylation reactions was investigated. Diastereomers 2,3,4 were separated by silica gel column chromatography. Based on NMR data, their configurations were discussed and tentatively determined, and their anti-cancer activity is under test.