| 齐多夫定的合成 |
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| 引用本文： | 陈发普,余宏宇.齐多夫定的合成[J].中国医药工业杂志,1996,27(11):483-485. |
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| 作者姓名： | 陈发普 余宏宇 |
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| 作者单位： | 中国人民解放军第二军医大学，美国辛辛那提大学，新亚药业公司药物研究所 |
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| 摘 要： | 以胸腺嘧啶脱氧核苷为原料，６位羟基经保护后，通过Ｍｉｔｓｕｎｏｂｕ反应以ＮａＮ_３取代同时发生构型转换接上叠氮基，然后脱去保护基制得齐多夫定，收率６１％。
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| 关 键 词： | 齐多夫定（AZT），合成 |
SYNTHESIS OF ZIDOVUDINE |
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| Authors: | CHEN Fa-Pu YU Hong-Yu LI Yun-Hu CHEN Fa-Kai WU Qiu-Ye |
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| Institution: | Second Military Medical University.Shanghai 200433;University of Cincinnati.U.S.A. |
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| Abstract: | Zidovudine(3'-azido-3'-deoxythymidine,AZT)was synthesized from thymidine(4).4 was transformed into 2,3'-anhydro- 5'-O-(4-methoxybenzoyl) thymidine(2) with diethyl azodicarboxylate,Ph3P and 4-MeOC6 H4CO2H by Mitsunobu reaction.2 was treated with NaN3 to afford 3'-azido-3'-deoxy-5'-O-(4-methoxybenzoyl) thymidine(3),followed by 5'-O-deprotetion to yield AZT.The overall yield was 61%. |
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| Keywords: | zidovudine(AZT) synthesis |
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