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| 1,3-二(乙氧基甲基)-5-N,N-二甲氨基-6-甲基尿嘧啶的合成 | |
| 引用本文： | 马小艳,王瑞平,李阿敏,陈艳丽,王孝伟,张志丽,刘俊义.1,3-二(乙氧基甲基)-5-N,N-二甲氨基-6-甲基尿嘧啶的合成[J].有机化学,2008,28(2):301-303. |
| 作者姓名： | 马小艳 王瑞平 李阿敏 陈艳丽 王孝伟 张志丽 刘俊义 |
| 作者单位： | 1. 北京大学药学院化学生物学系,北京,100083 2. 首都医科大学化学生物学与药学学院,北京,100069 3. 北京大学药学院化学生物学系,北京,100083;北京大学天然药物及仿生药物国家重点实验室,北京,100083;首都医科大学化学生物学与药学学院,北京,100069 |
| 基金项目： | 国家自然科学基金，面向21世纪教育振兴行动计划(985计划) |
| 摘 要： | 报道了1,3-二(乙氧基甲基)-5-N,N-二甲氨基-6-甲基尿嘧啶方便、高产率的合成方法. 以6-甲基尿嘧啶(1)为起始物, 经硝化、嘧啶N1,N 3-烷基化、还原及氨基甲基化, 首次高产率合成了1,3-二(乙氧基甲基)-5- N,N -二甲氨基-6-甲基尿嘧啶(5), 并对其化学结构进行了表征. |
| 关 键 词： | 1 3-二(乙氧基甲基)-5-N N-二甲氨基-6-甲基尿嘧啶 1 3-二(乙氧基甲基)-5-氨基-6-甲基尿嘧啶 5-硝基-6-甲基尿嘧啶 |
| 收稿时间： | 2007-04-12 |
| 修稿时间： | 2007-08-26 |
Synthesis of 1,3-(Diethoxymethyl)-5-N,N-dimethylamino-6-methyluracil |
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| MA Xiao-Yan,WANG Rui-Ping,LI A-Min,CHEN Yan-Li,WANG Xiao-Wei,ZHANG Zhi-Li,LIU Jun-Yi.Synthesis of 1,3-(Diethoxymethyl)-5-N,N-dimethylamino-6-methyluracil[J].Chinese Journal of Organic Chemistry,2008,28(2):301-303. | |
| Authors: | MA Xiao-Yan WANG Rui-Ping LI A-Min CHEN Yan-Li WANG Xiao-Wei ZHANG Zhi-Li LIU Jun-Yi |
| Institution: | ( Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100083)( State Key Laboratory of Natural and Biomimetic Drug, Peking University, Beijing 100083)( School of Chemical Biology and Pharmaceutical Sciences, Capital University, Beijing 100069) |
| Abstract: | A new practical approach to prepare 1,3-(diethoxymethyl)-5-N,N-dimethylamino-6-methyluracil (5) has been realized from 6-methyluracil (1). Compound 5 is a key intermediate material in the synthesis of HIV-1 RT and methionine synthase inhibitors. 6-Methyluracil (1) reacted with HNO3-P2O5 giving 5-nitro-6-methyluracil (2), which alky-lated at N1,N3 through reaction with ethoxymethyl chloride to give 3. Compound 3 was then reduced through treatment with HCOONH4-Pd/C and the derived C-5 amino group reacted with CH3I to convert into compound 5 in good yield. |
| Keywords: | 1 3-(diethoxymethyl)-5-N N-dimethylamino-6-methyluracil 1 3-(diethoxymethyl)-5-amino-6- methyluracil 5-nitro-6-methyluracil |
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