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Antifibrosis pyridinone compound and its preparing process

A technology for synthesizing pyridones and compounds, which is applied in the field of synthesis of pyridone compounds and improvement of synthetic process methods, can solve the problems of easy polymerization, difficult to obtain compounds, unstable compounds and the like, and achieves simple and easily controllable reaction process and wide adaptability. The effect of sexual and structural stability

Inactive Publication Date: 2005-09-14
HAIKOU PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Although the above-mentioned method has been further improved to some previous methods, the compound of (VI) formula is unstable and easily polymerized, and the compound of (VII) formula is not easy to obtain.

Method used

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  • Antifibrosis pyridinone compound and its preparing process
  • Antifibrosis pyridinone compound and its preparing process
  • Antifibrosis pyridinone compound and its preparing process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] In the 1-substituted phenyl-5-methyl-2(1H)pyridone of formula (I), n=1, R=Br, such as:

[0038] 1-(2-Bromophenyl)-5-methyl-2-(1H)pyridone;

[0039] 1-(3-Bromophenyl)-5-methyl-2-(1H)pyridone;

[0040] 1-(4-Bromophenyl)-5-methyl-2-(1H)pyridinone.

Embodiment 2

[0042] In the 1-substituted phenyl-5-methyl-2(1H)pyridone of formula (I), n=2, R=Br or Cl, such as:

[0043] 1-(2,3-Dibromophenyl)-5-methyl-2-(1H)pyridone

[0044] 1-(2,4-Dibromophenyl)-5-methyl-2-(1H)pyridone

[0045] 1-(2,5-Dibromophenyl)-5-methyl-2-(1H)pyridone

[0046] 1-(2,6-Dibromophenyl)-5-methyl-2-(1H)pyridone

[0047] 1-(3,4-Dibromophenyl)-5-methyl-2-(1H)pyridone

[0048] 1-(3,5-Dibromophenyl)-5-methyl-2-(1H)pyridone

[0049] 1-(2,3-Dichlorophenyl)-5-methyl-2-(1H)pyridone

[0050] 1-(2,4-Dichlorophenyl)-5-methyl-2-(1H)pyridone

[0051] 1-(2,5-Dichlorophenyl)-5-methyl-2-(1H)pyridone

[0052] 1-(2,6-Dichlorophenyl)-5-methyl-2-(1H)pyridone

[0053] 1-(3,5-Dichlorophenyl)-5-methyl-2-(1H)pyridone

Embodiment 3

[0055] In the 1-substituted phenyl-5-methyl-2(1H)pyridone of formula (I), n=1, R=trifluoromethyl, such as:

[0056] 1-(2-Trifluoromethylphenyl)-5-methyl-2-(1H)pyridone

[0057] 1-(4-Trifluoromethylphenyl)-5-methyl-2-(1H)pyridone

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Abstract

An antifibrosis pyridinone medicine, 1-polysubstituted phenyl-5-methyl-2(IH) pyridinone is prepared from 2-amino-5-methyl pyridine through diazotization reaction in polar solvent containing concentrated acid and sodium nitrate as diazotizing agent. Said concentrated acid may be inorganic acid or organic acid. Said polar solvent is glacial acetic acid or water. Its advantages are high antifibrosis effect, and simple reaction procedure.

Description

technical field [0001] The invention relates to a chemically synthesized compound for treating fibrotic diseases and a production process thereof, in particular to the synthesis of pyridone compounds for treating fibrotic diseases and the improvement of the synthetic process. technical background [0002] Fibrotic diseases such as renal fibrosis, liver cirrhosis, and myocardial fibrosis are important diseases that seriously endanger human life and health. With global industrialization and changes in people's lives and diets, the incidence of fibrotic diseases is gradually increasing. Correspondingly, many scholars at home and abroad have conducted a large number of researches on anti-fibrosis compounds from different fields such as chemical compounds, natural compounds, biological agents, and gene therapy for the pathogenesis of fibrosis. So far, pyridones have been found to be an effective class of anti-fibrotic compounds. [0003] US Pat. No. 3,839,346 and US Pat. No. 4,0...

Claims

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Application Information

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IPC IPC(8): A61K31/4418A61P43/00C07D213/90
Inventor 陶立坚胡高云谭桂山
Owner HAIKOU PHARMA FACTORY
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