| 四环素C-2位Mannich反应的研究 |
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| 引用本文： | 王洪涛,周站云,王瑞平,王孝伟,刘俊义. 四环素C-2位Mannich反应的研究[J]. 化学通报, 2006, 69(7): 536-539 |
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| 作者姓名： | 王洪涛 周站云 王瑞平 王孝伟 刘俊义 |
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| 作者单位： | 北京大学药学院化学生物学系,北京,100083;首都医科大学化学生物学与药学院,北京,100054 |
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| 摘 要： | 报道了四环素C-2位与伯胺、仲胺反应形成Mannich碱的简便方法:四环素盐酸盐在甲醇和水溶液中与伯胺反应,生成二级Mannich碱;四环素在叔丁醇中与仲胺反应,生成三级Mannich碱。合成了10个化合物,其中8个未见报道,并对所合成化合物的结构进行了表征。
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| 关 键 词： | 四环素 合成 神经保护 Mannich反应 |
| 收稿时间： | 2005-02-23 |
| 修稿时间： | 2005-02-232006-01-19 |
Mannich Reaction at C-2 of Tetracyclines |
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| Wang Hongtao,Zhou Zhanyun,Wang Ruiping,Wang Xiaowei,Liu Junyi. Mannich Reaction at C-2 of Tetracyclines[J]. Chemistry, 2006, 69(7): 536-539 |
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| Authors: | Wang Hongtao Zhou Zhanyun Wang Ruiping Wang Xiaowei Liu Junyi |
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| Affiliation: | 1.Department of Chemieal Biology, School of Pharmaeeutieal Seienees, Peking University, Beijing 100083 ; 2.School of Chemieal Biology and Pharmaeeutieal Seienees, Capital University of Medieal Seienees, Beijing 100054 |
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| Abstract: | A simple method for synthesis of tetracycline Mannich bases by C-2 reacting with primary and secondary amine was reported. Secondary Mannich base was obtained by primary amine reacting with tetracycline hydrochloride in methanol and water. Tertiary Mannich base was obtained by the reaction of secondary amine and tetracycline in t-butanol. The structures of synthesized ten of tetracyline analogs 4 - 13 had been identified. |
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| Keywords: | Tetracycline Synthesis Neuroprotective Mannich reaction |
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