应用化学 ›› 2011, Vol. 28 ›› Issue (04): 382-386.DOI: 10.3724/SP.J.1095.2011.00372

• 研究论文 • 上一篇    下一篇

4-取代-2-氨基嘧啶衍生物的合成

陈启凡*,张慧东,宫胜臣   

  1. (辽东学院实验中心 丹东 118003)
  • 收稿日期:2010-06-25 修回日期:2010-09-16 出版日期:2011-04-10 发布日期:2011-04-10
  • 通讯作者: 陈启凡,教授; Tel:0415-3789877; Fax:0415-3789873; E-mail:qifan_c405@163.com; 研究方向:精细化工中间体的合成
  • 基金资助:
    “十五”国家科技攻关计划(2004BA304B)

Synthesis of 4-Substituted-2-amino-pyrimidines

CHEN Qifan*, ZHANG Huidong, GONG Shengchen   

  1. (Experiment Center,Eastern Liaoning University,Dandong 118003)
  • Received:2010-06-25 Revised:2010-09-16 Published:2011-04-10 Online:2011-04-10

摘要:

含乙酰基的芳杂环类化合物分别与过量40%~50%的N,N-二甲基甲酰胺-二甲基缩醛(DMF-DMA)在回流温度下进行反应,得到相应的中间产物3-(二甲氨基)-1-(取代)-2-丙烯-1-酮,收率为71.2%~85.2%。 所得中间产物在乙醇介质中,在乙醇钠存在下与盐酸胍回流反应5~7 h,制备了14个4-取代-2-氨基嘧啶类化合物,收率达66.6%~86.1%,产物经核磁、质谱、元素分析等进行了表征。

关键词: 取代氨基嘧啶, 合成, 表征

Abstract:

N,N-Dimethylformamide-dimethyl acetal(DMF-DMA) was refluxed with the corresponding aromatic or heterocyclic compounds to prepare the intermediates 3-(dimethylamino)-1-(substituted)prop-2-en-1-one with a yield of 71.2%~85.2%. By refluxing the obtained intermediates with guanidine hydrochloride in ethanol and in the presence of sodium ethoxide, fourteen 4-substituted-2-amino-pyrimidines were obtained in good yield of 66.6%~86.1%. All the products were confirmed by NMR, mass spectrometry, and elemental analysis.

Key words: substituted-amino-pyrimidines, synthesis, characterization

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