有机化学 ›› 2014, Vol. 34 ›› Issue (7): 1437-1441.DOI: 10.6023/cjoc201401020 上一篇    下一篇

研究论文

CuBr2催化的三组分反应合成喹啉-2,4-二羧基衍生物

王扣, 于浩飞, 丁林芬, 胡建林   

  1. 昆明医科大学药学院暨云南省天然药物药理重点实验室 昆明 650500
  • 收稿日期:2014-01-13 修回日期:2014-03-12 出版日期:2014-07-25 发布日期:2014-04-15
  • 通讯作者: 胡建林 E-mail:hujlkm@sina.com
  • 基金资助:

    云南省科技厅应用基础研究计划(No.2011FZ097)资助项目.

CuBr2-Catalyzed Three-Component Coupling for Synthesis of Quinoline-2,4-dicarboxyl Derivatives

Wang Kou, Yu Haofei, Ding Linfen, Hu Jianlin   

  1. School of Pharmaceutical Science and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500
  • Received:2014-01-13 Revised:2014-03-12 Online:2014-07-25 Published:2014-04-15
  • Supported by:

    Project supported by the Applied Basic Research Plan of Yunnan Province Science and Technology Department (No. 2011FZ097).

以廉价的CuBr2为催化剂,发展了一种通过芳胺、乙醛酸酯与丙酮酸酯三组分反应制得喹啉-2,4-二羧基衍生物的简便有效方法. 该方法具有很好的原子经济性,使用了便宜的催化剂和易得的试剂,在温和的条件下解决了以往喹啉-2,4-二羧基衍生物合成条件苛刻、产率低等问题,在生物活性分子和药物分子合成上有潜在的应用价值.

关键词: 喹啉-2,4-二羧基衍生物, 芳胺, 乙醛酸酯, 丙酮酸酯, CuBr2

A convenient and efficient method for synthesizing quinoline-2,4-dicarboxyl derivatives has been developed via a simple one-pot reaction of aromatic amines, glyoxylic ester, and pyruvate using low-costing CuBr2 as a catalyst. The method is atom efficiency, and utilizes non-expensive catalysts and easily available reagents, which provides an attractive approach to quinoline-2,4-dicarboxyl derivatives. This process has potential applications in the synthesis of biologically and medicinally relevant compounds.

Key words: quinoline-2,4-dicarboxyl derivatives, aromatic amines, glyoxylic ester, pyruvate, CuBr2