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报道以肌苷、Me3SiCl、KCN等为原料制备 2 β D 呋喃核糖 4 硒唑羧酰氨 (1)的方法 .以肌苷为原料 ,制备 1 O 乙酰基 2 ,3 ,5 三 O 苯甲酰基 β D 呋喃核糖 (5 ) .在NaI催化下 ,Me3SiCl与KCN作用得到含Me3SiCN的混合物 ,其液相部分在SnCl4 催化下直接与 (5 )反应得到 1 氰基 2 ,3 ,5 三 O 苯甲酰基 β D 呋喃核糖 (4 ) .氰糖 (4 )在乙醇中依次用现制的H2 Se及溴代丙酮酸乙酯处理 ,得到 2 (2 ,3,5 三 O 苯甲酰基 β D 呋喃核糖 ) 4 硒唑羧酸乙酯 (3) .硒唑 (3)经NaOMe脱保护及氨化后得到化合物 (1) .腹腔注射 (1) ,对小鼠EAC及L12 10有明显的抑制作用 ,(1)表现出较高的抗肿瘤活性
A method for preparing 2β-D ribofuranose 4selenazolecarboxamides (1) using inosine, Me3SiCl and KCN as starting materials was reported.Iomyosin was used as a starting material to prepare 1 O acetyl 2,3,5-tri-O-benzoyl β D ribofuranose (5). Under the catalysis of NaI, the reaction of Me3SiCl with KCN to obtain a mixture containing Me3SiCN, the liquid part of SnCl4 catalysis directly with (5) to give 1 cyano 2, 3, The acyl β D ribofuranose (4). Cyanide (4) was treated sequentially with H 2 Se and ethyl bromopyruvate in ethanol to give 2 (3,5,6-tri-O-benzoyl β D ribofuranose ) (4) Selenazolone ethyl ester (3) Selenazol (3) Compound (1) was obtained after deprotection and amination of NaOMe.The peritoneal injection (1) (1) showed higher anti-tumor activity