| 胞苷的合成 |
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| 引用本文： | 李永,渠桂荣,刘启宾,韩素辉.胞苷的合成[J].精细化工,2004,21(12):917-919. |
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| 作者姓名： | 李永 渠桂荣 刘启宾 韩素辉 |
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| 作者单位： | 河南师范大学,化学与环境科学学院,河南,新乡,453007 |
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| 基金项目： | 国家自然科学基金资助项目(No.20372018) |
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| 摘 要： | 在微波辐射和无溶剂条件下,以2,4 二乙氧基嘧啶(Ⅰ)和四乙酰核糖(Ⅱ)为原料,对甲苯磺酸为催化剂进行缩合,得到中间体4 乙氧基 (2′,3′,5′ 三 O 乙酰基)尿苷(Ⅲ),收率76%,随后通过氨-甲醇一步氨解,得到胞苷(Ⅳ),收率83%,胞苷总收率63%;Ⅲ和Ⅳ的结构经1HNMR和13CNMR证实。最佳缩合条件是n(Ⅰ)∶n(Ⅱ)=1 4∶1,对甲苯磺酸的用量为0 1g/gⅡ,280W微波辐射4min;最佳氨解条件是在110℃反应12h。
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| 关 键 词： | 胞苷 2 4-二乙氧基嘧啶 四乙酰核糖 微波辐射 |
| 文章编号： | 1003-5214(2004)012-0917-03 |
Synthesis of Cytidine |
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| LI Yong,QU Gui-rong,LIU Qi-bin,HAN Su-hui.Synthesis of Cytidine[J].Fine Chemicals,2004,21(12):917-919. |
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| Authors: | LI Yong QU Gui-rong LIU Qi-bin HAN Su-hui |
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| Affiliation: | LI Yong,QU Gui-rong~*,LIU Qi-bin,HAN Su-hui |
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| Abstract: | Condensation of 2,4-diethoxypyrimidine(Ⅰ)and tetraacetylribofuranose(Ⅱ)in the presence of TsOH as catalyst under microwave irradiation and without solvent gave 4-ethoxy-(2′,3′,5′-tri-O-acetyl)uridine(Ⅲ) in 76% yield.Cytidine(Ⅳ)was obtained in 83% yield by treatingⅢ with NH_3-CH_3OH.The total yield of Ⅳ was 63%.Structures of Ⅲ and Ⅳ were confirmed with ~1HNMR and ~(13)CNMR.The best conditions for condensation was n(Ⅰ)/n(Ⅱ)=1.4,0.1 g TsOH/g Ⅱ and 280 W microwave irradiation for 4 min.The best condition for aminolysis was 110 ℃ for (12 h.) |
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| Keywords: | cytidine 2 4-diethoxypyrimidine tetraacetylribofuranose microwave irradiation |
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