节点文献
1,3-二(乙氧基甲基)-5-N,N-二甲氨基-6-甲基尿嘧啶的合成
Synthesis of 1,3-(Diethoxymethyl)-5-N,N-dimethylamino-6-methyluracil
【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,N3-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.
【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 alkylated 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.
【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；
【Key words】 1,3-(diethoxymethyl)-5-N,N-dimethylamino-6-methyluracil； 1,3-(diethoxymethyl)-5-amino-6-methyluracil； 5-nitro-6-methyluracil；
【Key words】 1,3-(diethoxymethyl)-5-N,N-dimethylamino-6-methyluracil； 1,3-(diethoxymethyl)-5-amino-6-methyluracil； 5-nitro-6-methyluracil；
【基金】 国家自然科学基金(No.20672008);教育部“985”计划资助项目
- 【文献出处】 有机化学 ,Chinese Journal of Organic Chemistry , 编辑部邮箱 ,2008年02期
- 【分类号】TQ463.53
- 【被引频次】2
- 【下载频次】224