4-Hydroxy-2-quinolones. 154*. Pyrimidin- 2-ylamides of 1-r-4-hydroxy-2-oxo-1,2-dihydro- quinoline-3-carboxylic acids. synthesis, structure, and properties

被引:0
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作者
I. V. Ukrainets
A. A. Tkach
L. A. Grinevich
A. V. Turov
O. V. Bevz
机构
[1] National University of Pharmacy,
[2] Taras Shevchenko National University,undefined
来源
Chemistry of Heterocyclic Compounds | 2009年 / 45卷
关键词
2-aminopyrimidine; 1-R-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides; bromina-tion; antitubercular activity; X-ray structural analysis;
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摘要
The synthesis of a series of 1-R-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acids pyrimidin-2-ylamides has been carried out with the aim of subsequent microbiological investigation. In acetic acid it was found that these compounds are brominated by 1 equivalent of bromine at position 5 of the pyrimidine ring. The only exception is the 1-allyl derivative which undergoes heterocyclization under these conditions to give 2-bromomethyl-5-oxo-1,2-dihydro-5H-oxazolo[3,2-a]quinoline-4-carboxylic acid pyrimidin-2-ylamide. The results of a study of the antitubercular activity of the synthesized compounds are presented.
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页码:567 / 579
页数:12
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