2-(N,N二-乙基氨基)-1,3,2二-氧磷杂环戊烷与羟烷基替加氟及硫反应得中间体2,三乙胺对2开环得内盐式磷酯替加氟缀合物3。2和3的结构经1H NMR,31P NMR和元素分析表征。初步抗癌活性测试结果表明,3对膀胱癌细胞T-24与胃癌细胞BGC-823有一定的抑制作用。
Intermediate 2 was synthesized by one-pot reaction of 2-(N,N-diethylamino)-1,3,2-dioxaphospholane and N1-(2-furanidyl)-N3-(hydroxyalkyl)-5-fluyorouracil and sulfur.2 reacted with triethylamine to obtain conjugate of phosphate zwitterions and tegafur(3).The structures of 2 and 3 were confirmed by 1H NMR,31P NMR and elemental analysis.3 exhibited antitumor activity against human urinaryl bladder cancer cell T-24 and stomach cancer cell BGC-823.