化学学报 ›› 1983, Vol. 41 ›› Issue (5): 475-478. 上一篇    

研究论文

7-取代-4-喹诺酮-2-羧酸甲酯的合成

梁晓天;李河水   

  1. 中国医学科学院药物研究所
  • 发布日期:1983-05-15

The synthesis of methyl 7-substituted-4-quinolone-2- carboxylate

LIANG XIAOTIAN;LI HESHUI   

  • Published:1983-05-15

关键词: 羧酸酯, 喹啉酮 P

When m-aminophenol and m-phenylenediamine were allowed to react with dimethyl acetylenedicarboxylate at room temperature, both addition and cyclization occurred, although in low yields, giving methyl 7-hydroxy-4-quinolone-2-carboxylate (2) and methyl 7-amino- 4-quinolone-2-carboxylate (3) respectively. The use of rather drastic conditions (heating in diphenyl ether) for similar cyclizations was not needed here, due to the activating influence of the amino and hydroxy functionalities in para relationship with the site of ring closure. We also prepared some acylated derivatives 5-8.

Key words: CARBOXYLIC ACID ESTER, QUINOLINONE P

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