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2-substituted quinolone compound and use in pharmacy

A technology of compounds and general formulas, applied in the field of pharmaceuticals, can solve problems such as undisclosed quinolones

Inactive Publication Date: 2009-05-20
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the compound that quinolone 2-position is substituted by benzimidazole, benzoxazole and benzothiazole is not disclosed, and whether the compound that these quinolone 2-position is substituted by benzimidazole, benzoxazole and benzothiazole has Antitumor activity reported

Method used

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  • 2-substituted quinolone compound and use in pharmacy
  • 2-substituted quinolone compound and use in pharmacy
  • 2-substituted quinolone compound and use in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Preparation of Diethyl Butanonedioate

[0052] Add absolute ethanol (50ml) and sodium (10g, 0.435mol) to a 500ml three-necked flask equipped with a reflux condenser and a drying tube, and heat to reflux until the sodium disappears after the reaction is slightly slow. Change the reflux device to a distillation device, evaporate the ethanol to dryness under reduced pressure, and release the vacuum after cooling to room temperature. Add anhydrous ether (80ml) and stir to form a paste, cool to below -5°C, slowly add diethyl oxalate (58.23ml, 0.427mol) and ethyl acetate (39.3ml, 0.401mol) dropwise below -5°C Mixture. Stirring was continued for 1 hour, then the temperature was raised to 38-40° C., refluxed for 1 hour, and left overnight. Neutralize to pH 1-2 with 10% sulfuric acid at low temperature, separate the ether layer, wash with water several times, wash with saturated sodium bicarbonate solution three times, then wash with saturated brine, anhydrous Na 2 SO 4 dry....

Embodiment 2

[0054] 1,4H-quinolin-4-one-2-carboxylic acid ethyl ester

[0055] Aniline (14g, 0.15mol), diethyl butanonedioate (29g, 0.154mol), and benzene (20ml) were added to the reaction flask, and refluxed for 3 hours under nitrogen protection. Benzene was recovered, and silica gel column chromatography was carried out using a mixed solvent of ethyl acetate and petroleum ether as a developing solvent to obtain a yellow liquid. The resulting yellow liquid was mixed with diphenyl ether (60ml), heated to reflux and kept at that temperature for 1 hour. After cooling, a pale yellow solid was precipitated, filtered, washed with petroleum ether, and dried to obtain 11.7 g of the product, yield 35.9%, mp 209-211°C.

Embodiment 3

[0057] 1,4H-quinolin-4-one-2-carboxylic acid

[0058] A mixture of ethyl 1,4H-quinolin-4-one-2-carboxylate (11.5 g, 0.053 mol), sodium hydroxide (4.24 g, 0.016 mol), and water (57 ml) obtained in Example 2 was refluxed for 2 hours. Cool, filter, wash with water, and dry to obtain 9.1 g of off-white powder, yield 90.8%, mp 279°C.

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PUM

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Abstract

A 2-bit substituted quinonone compound and its use in pharmacy are disclosed. It has antineoplastic activity and can be used for antineoplastic medicine.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a novel 2-position substituted quinolone compound, and also relates to the application of the compound in the preparation of antitumor drugs. Background technique [0002] In recent years, it has been reported in the literature that quinolones have good antitumor activity and have multiple targets. According to literature reports, benzimidazole, benzoxazole and benzothiazole compounds may have topoisomerase I inhibitory activity. But the compound that quinolone 2-position is substituted by benzimidazole, benzoxazole and benzothiazole is not disclosed, and whether the compound that these quinolone 2-position is substituted by benzimidazole, benzoxazole and benzothiazole has Antitumor activity reported. Contents of the invention [0003] The object of the present invention is to provide a new anti-tumor active quinolone 2-position substituted by benzimidazole, benzoxazole and benzothiazole...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/04C07D413/04C07D417/04A61K31/4709A61P35/00
Inventor 李志裕尤启冬何训贵
Owner CHINA PHARM UNIV
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