| 齐多夫定合成改进 |
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| 引用本文： | 李伟,姜玉钦,黎敏霞,郝二军.齐多夫定合成改进[J].河南师范大学学报(自然科学版),2004,32(4):136-137,143. |
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| 作者姓名： | 李伟 姜玉钦 黎敏霞 郝二军 |
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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;北华大学,基础部,吉林,吉林,132001 |
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| 摘 要： | 以胸苷为原料,5′位醇羟基用对甲氧基苯甲酸成酯保护,然后与偶氮二甲酸二乙酯和三苯基膦反应成"氧桥",再与叠氮化钠反应引入"叠氮"基团,最后脱保护得齐多夫定,总收率为67%.本法在最后一步脱保护基后用碱性去离子水除杂,用热正丁醇纯化产物,操作简单,适宜工业化生产.
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| 关 键 词： | 齐多夫定 胸苷 合成 |
| 文章编号： | 1000-2367(2004)04-0136-02 |
An improved synthetic process of zidovudine |
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| LI Wei,JIANG Yu-qin,LI Min-xia,HAO Er-jun.An improved synthetic process of zidovudine[J].Journal of Henan Normal University(Natural Science),2004,32(4):136-137,143. |
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| Authors: | LI Wei JIANG Yu-qin LI Min-xia HAO Er-jun |
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| Institution: | LI Wei~1,JIANG Yu-qin~1,LI Min-xia~2,HAO Er-jun~1 |
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| Abstract: | Zidovudine was synthesized from thymidine.Thymidine was esterificated with 4-methoxybenzoic acid to protect its primary hydroxyl group of 5′ position and then was converted into 2,3′-anhydro-5′-o-(4-methoxybenzoyl)thymidine with diethyl azodicarboxylate and triphenylphosphine. 2,3′-anhydro-5′-o-(4-methoxybenzoyl) thymidine was treated with sodium azide to get 3′-azido-3′-deoxy-5′ -o-(4-methoxybenzoyl)thymidine, followed by 5′-o-deprotection to yield zidovudine in overall yield of 67%.After deprotection, impurities were removed with alkaline de-ionized water and zidovudine was purified by hot n-butyl alcohol. The method is simple and suitable for industrialization. |
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| Keywords: | zidovudine thymidine synthesis |
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