| 三氮唑核苷的合成 |
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| 引用本文： | 罗晓燕,殷斌烈,叶宗红.三氮唑核苷的合成[J].精细化工,2001,18(1):27-28. |
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| 作者姓名： | 罗晓燕 殷斌烈 叶宗红 |
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| 作者单位： | 1. 武汉化工学院"制药系,
2. 北京第二制药厂"信息部, |
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| 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 %。
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| 关 键 词： | 三氮唑核苷 1 2 3 5-O-四乙酰-βD-呋喃核糖 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 |
| 文章编号： | 1003-5214(2001)01-0027-02 |
Synthesis of Ribavirin |
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| LUO Xiao-yan,YIN Bin-lie,YE Zhong-hong.Synthesis of Ribavirin[J].Fine Chemicals,2001,18(1):27-28. |
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| Authors: | LUO Xiao-yan YIN Bin-lie YE Zhong-hong |
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| Affiliation: | LUO Xiao yan\+1,YIN Bin lie\+1,YE Zhong hong\+2 |
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| 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 CF3SO2OSi(CH3)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%. |
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| Keywords: | ribavirin 1 2 3 5 tetra O acetyl β D ribofuranose 1 (2 3 5 tri O acetyl β D ribofuranosyl) 1 2 4 triazole 3 carboxylic acid methyl ester |
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