摘要
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 ） -Ns- （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.
出处
《合成化学》
CAS
CSCD
2007年第2期192-194,共3页
Chinese Journal of Synthetic Chemistry
基金
国家自然科学基金资助项目(20372020)
关键词
替加氟
内盐式磷酸酯
合成
抗癌活性
tegafur
phosphate zwitterions
synthesis
antitumor activity
