5-(Substituted thiomethyl)-6-carbamoyluracils (IIIb-h) and 5-(substituted thiomethyl)-uracils (Va-h) were prepared and their ability to inhibit the growth of L-1210 cells in vitro was examined. The reaction of silylated furo [3, 4-d] pyrimidine-2, 4, 7 (1H, 3H, 5H)-trione (VI) with 1-O-acetyl-2, 3, 5-tri-O-benzoyl-β-D-ribofuranose (VII) in acetonitrile in the presence of SnCl4 gave 1-(2, 3, 5-tri-O-benzoyl-β-D-ribofuranosyl) furo [3, 4-d] pyrimidine-2, 4, 7 (1H, 3H, 5H)-trione (VIII) in 81.0% yield. The protected nucleoside (VIII) was hydrolyzed by sodium methoxide to give the N1-nucleoside (X).
5-(取代
硫甲基)-6-
氨基尿
嘧啶衍
生物 (IIIb-h) 和 5-(取代
硫甲基)-尿
嘧啶衍
生物 (Va-h) 被合成,并测试了它们在体外抑制 L-1210 细胞生长的能力。
硅化的
呋喃 [3, 4-d]
嘧啶-2, 4, 7 (1H, 3H, 5H)-三酮 (VI) 与 1-O-acetyl-2, 3, 5-tri-O-benzoyl-β-
D-核糖 (VII) 在
氯化锡 (SnCl4) 存在下于
乙腈中反应,得到了1-(2, 3, 5-tri-O-benzoyl-β-
D-核糖苷)
呋喃[3, 4-d]
嘧啶-2, 4, 7 (1H, 3H, 5H)-三酮 (VIII),产率为81.0%。该保护核苷 (VIII) 经甲基
钠水解后得到 N1-核苷 (X)。