3-甲基丁基氯甲酸酯置于potassium Carbonate,Sodium Hydroxide体系中,用 丙酮 用作溶剂,化学反应 2.0H,反应生成5'-脱氧-5-氟-N-[(3-甲基丁)羰基]胞苷
参考文献:Synthesis And Biological Activity Evaluation Of Cytidine-5'-Deoxy-5-Fluoro-N-[(Alkoxy/aryloxy)] Carbonyl-Cyclic 2',3'-Carbonates
标题:Synthesis And Biological Activity Evaluation Of Cytidine-5'-Deoxy-5-Fluoro-N-[(Alkoxy/aryloxy)] Carbonyl-Cyclic 2',3'-Carbonates
摘要:Capecitabine,An Oral Prodrug Of 5-Fu Was Developed To Improve The Tumor Selectivity And Tolerability. To Enhance The Efficacy Of Capacitabine,A Series Of 5'-Deoxy-5-Fluorocytidine Derivatives 5A-E Were Synthesized. In The Present Study,We Investigated Antitumor Activity Of 5'-Deoxy-5-Fluorocytidine Derivatives Both In Vivo And In Vitro Methods. Title Compounds Were Non-Mutagenic To Salmonella Typhimurium Tester Strain In Ames Test. Compounds 5D And 5E Are Potent To Inhibit The Proliferation Of Nci-69,Pz-Hpv-7,Mcf-7 And Hela Cells In Mu Assay. In Particular,5D And 5E Showed Potent Antitumor Activities Against L1210 Leukemia Cell Line. Collectively,These Findings Suggest That 5D And 5E Are More Potent Anti-Cancer Compounds Than Capecitabine. Published By Elsevier Masson Sas.
Doi:10.1016/j.Ejmech.2012.06.023