【摘要】 肌苷与醋酐〔n(肌苷 )∶n(醋酐 ) =1 0 0∶2 .18〕在催化剂对甲基苯磺酸的催化作用下制得 1,2 ,3,5 O 四乙酰 β D 呋喃核糖 (Ⅰ) ,收率为 84%。1,2 ,4 三氮唑 3 羧酸甲酯与N ,O 二 (三甲基硅烷基 )乙酰胺在乙腈中硅烷化反应后 ,直接与Ⅰ在催化剂CF3SO2 OSi(CH3) 3的作用下缩合〔n(1,2 ,4 三氮唑 3 羧酸甲酯 )∶n(Ⅰ)∶n(催化剂 ) =1∶1∶2〕制得 1 (2 ,3,5 三 O 乙酰基 β D 呋喃核糖基 ) 1,2 ,4 三氮唑 3 羧酸甲酯 (Ⅱ) ,收率为 83 4% ,Ⅱ经氨解制得三氮唑核苷。总收率为 5 5 6 %。更多还原

【Abstract】 Inosine was acetylated with acetic anhyclride(mol ratio 1 00∶2 18) in the presence of the catalyst p toluenesulfonic acid to give 1,2,3,5 tetra O acetyl β D ribofuranose(Ⅰ)in 84% yield.1,2,4 Triazole 3 carboxylic acid methyl ester was silylated with N,O bis(trimethylsilyl)acetamide in acetonitrile,and then directly condensed with Ⅰ in the presence of the catalyst CF 3SO 2OSi(CH 3) 3 [mol ratio n (1,2,4 triazole 3 carboxylic acid )∶ n (Ⅰ)∶ n (catalyst)=1∶1∶2)]to give 1 (2,3,5 tri O acetyl β D ribofuranosyl) 1,2,4 triazole 3 carboxylic acid methyl ester(Ⅱ)in 83 4% yield.Ⅱ was ammonolyzed to produce ribavirin.The overall yield was 55 6%.更多还原