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Production of pyriphenanthrenone as anti-fibrosis medicine

A pirfenidone and anti-fibrosis technology, applied in the new field of organic chemical synthesis, can solve the problems of unsuitable industrial production, long preparation method, expensive and the like

Inactive Publication Date: 2006-08-16
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The above-mentioned preparation method is long, the steps are cumbersome, and the raw materials and reagents used in the reaction are more expensive, so it is not suitable for domestic industrial production

Method used

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  • Production of pyriphenanthrenone as anti-fibrosis medicine
  • Production of pyriphenanthrenone as anti-fibrosis medicine
  • Production of pyriphenanthrenone as anti-fibrosis medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0036] (a).5-Methyl-2(1H)pyridone

[0037] 10.80 g of 2-amino-5-picoline and 250 ml of 5% sulfuric acid were successively added into the three-necked flask, and an aqueous solution of sodium nitrite (12.00 g) was added dropwise at 0-5° C.; then, the reaction solution was heated and hydrolyzed. After completion of the reaction, neutralize with sodium carbonate, concentrate and dry under reduced pressure to obtain a brownish-yellow solid, which is the crude product of 5-methyl-2(1H)pyridone; recrystallize from absolute ethanol to obtain 7.90 g of light yellow crystals, with a yield of 72.5% , mp182-183°C (literature mp181-182°C). IR (cm -1 ): 2842.7, 2840.0 (N-H), 1657.0 (C=O), 1145.1 (C-N). 1HNMR (δppmCDCl3): 2.10 (3H, s, 5-CH3), 6.53 (1H, d, H-3), 7.17 (1H, d, H-4), 7.33 (1H, d, H-6), 13.52 (1H, s, N-H).

[0038] (b). Pirfenidone

[0039] 5.45 g of 5-methyl-2(1H) pyridone, 7.66 g of anhydrous potassium carbonate, 20 g of iodobenzene, and 0.16 g of cuprous chloride were su...

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Abstract

Production of anti-fiberization medicine pyphenitone is carried out by taking 2-amino-5-picoline as initial materials, diazotizing, hydrolyzing to obtain 5-methyl-amino-2(1H)pyridone, nucleophilic substituting benzene halide with under existence of catalyst and purifying to obtain final product. It is cheap, has short reactive time and more yield. It can be used for industrial production.

Description

technical field [0001] The invention relates to a new organic chemical synthesis method, in particular to a preparation method of pirfenidone, an anti-fibrosis drug for treating fibrosis diseases. Background technique [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 drugs from different fields such as chemical drugs, natural drugs, biological agents, and gene therapy for the pathogenesis of fibrosis. So far, pyridone compounds have been found to be a A class of effective anti-fibrosis compounds, among which, pirfenidone is the representative compound, which has been studied abroad for many years and i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/64
Inventor 马臻王尊元
Owner ZHEJIANG ACAD OF MEDICAL SCI
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