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Salt of quinoline derivative

A quinoline and drug technology, applied in 3--5--7-trifluoromethyl-quinoline organic acid salt and its pharmaceutical application field, can solve adverse reactions, unsatisfactory treatment effects, drug resistance and the like problems to achieve practical therapeutic activity

Inactive Publication Date: 2013-05-29
SHANGHAI YIZHI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] For now, although there are many kinds of drugs for the treatment of cancer, these existing drugs are likely to cause multiple and severe adverse reactions, and some produce drug resistance, and the therapeutic effect of the existing drugs is still not ideal.

Method used

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  • Salt of quinoline derivative
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Examples

Experimental program
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Effect test

Embodiment 1

[0049] 3-(4-Acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7-trifluoromethyl-quinoline fumarate

[0050] Compound 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7-trifluoromethyl-quinoline 47.3 grams (0.1mol) and fumaric acid 11.7 ( 0.1mol) gram dissolved in 1000ml of boiling ethanol. The hot solution was filtered through diatomaceous earth, then slowly cooled under gentle stirring, and stood at a temperature of 0-5°C for several hours to precipitate 3-(4-acetylazin-1-yl)-5-(3 -Nitrobenzylamino)-7-trifluoromethyl-quinoline fumarate crystals, 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino )-7-trifluoromethyl-quinoline fumarate crystals, washed with ethanol and dried under vacuum at 50°C, yielding 57.9 g of product.

Embodiment 2

[0052] 3-(4-Acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7-trifluoromethyl-quinoline fumarate

[0053] Compound 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7-trifluoromethyl-quinoline fumarate 47.8 grams and fumaric acid 11.7 grams Stir in 1000 ml of refluxing ethanol until all solids are dissolved. Add activated carbon, filter the hot solution through diatomaceous earth, and cool down to room temperature while stirring. Standing for several hours in a temperature environment of 0-5°C, 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7-trifluoromethyl-quinolin phenoline fumarate crystals, 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7-trifluoromethyl-quinoline fumarate crystals were filtered off , washed with ethanol and dried under vacuum at 50°C to yield 57.2 g of product.

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Abstract

The invention relates to fumarate of 3-(4-acetyl piperazine-1-yl)-5-(3-nitryl benzyl amino)-7-trifluoromethyl-quinoline and a derivative or a pharmaceutically acceptable solvates of fumarate and an application of fumarate in preparation of a medicine for treating cancer.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7-trifluoromethyl-quinoline Organic acid salts and their pharmaceutical applications. Background technique [0002] For now, although there are many kinds of drugs for treating cancer, these existing drugs are likely to cause multiple and severe adverse reactions, and some produce drug resistance, and the therapeutic effect of the existing drugs is still not ideal. Chinese patent application publication number CN 101993416A describes some active compounds for treating cancer. Contents of the invention [0003] The present invention discloses some new compounds, preparation methods of these compounds, pharmaceutical compositions containing these compounds and pharmaceutical applications of these compounds and compositions. [0004] These compounds exhibit good water solubility stability and solid for...

Claims

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Application Information

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IPC IPC(8): C07D215/38A61K31/496A61P35/00
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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