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Novel method for preparing 5-methyl-1-phenyl-2-(1H)-pyridone

A technology of pyridone and methyl, applied in the field of preparation of 5-methyl-1-phenyl-2--pyridone, achieving the effects of good product quality, increased yield, and small residue

Inactive Publication Date: 2010-11-24
BEIJING KAWIN TECH SHARE HLDG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Currently, there are no drugs sold specifically for the treatment of IPF on the market

Method used

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  • Novel method for preparing 5-methyl-1-phenyl-2-(1H)-pyridone
  • Novel method for preparing 5-methyl-1-phenyl-2-(1H)-pyridone

Examples

Experimental program
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Embodiment 1

[0024] Put 4.4kg of 5-methyl-2(1H)-pyridone, 11.3kg of bromobenzene, 144g of ketone bromide, and 6.08kg of anhydrous potassium carbonate into a 50L reactor, slowly raise the temperature to reflux, and maintain reflux React for 12 hours, stop the reaction, concentrate under reduced pressure (recover bromobenzene), after recovery, cool down slightly, add 15L of distilled water, cool to 0-5°C, stir and crystallize for 2 hours, filter, drain the filter cake, wash with distilled water (5L ×3), put in a reaction kettle, slowly add dilute hydrochloric acid, stir to dissolve, add 1% activated carbon, decolorize at about 50°C for about 15 minutes, filter, cool the filtrate, slowly add saturated NaOH solution to the filtrate until the pH value is about 14. Lower the temperature, stir and crystallize, filter, drain the filter cake, wash with distilled water (5L×3), and dry to dryness at 80°C to obtain 5.5kg of crude product.

[0025] Heat 5.5kg of crude pirfenidone, 70L of distilled wate...

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Abstract

The invention provides a novel method for preparing 5-methyl-1-phenyl-2-(1H)-pyridone. The method is characterized in that: bromobenzene which is one of reaction raw materials is used as a reaction solvent; and water is used as a crystallization and recrystallization solvent of the product. The product has the advantages of high yield, high purity, less pollution, and suitability for industrialized production.

Description

Technical field: [0001] The present invention relates to a new preparation method of 5-methyl-1-phenyl-2-(1H)-pyridone technical background: [0002] Idiopathic pulmonary fibrosis (IPF) is a common disease all over the world, and its morbidity and mortality have increased in the past 10 years. It is estimated that the number of patients suffering from IPF in the United States, Europe and Japan is about 220,000 , of which there are 90,000 IPF patients in the United States. IPF is comparable in prevalence to diseases such as chronic myelogenous leukemia (CML). The disease is a progressive disease. The development of secondary pulmonary fibrosis is relatively slow, and the development of pulmonary fibrosis can stop after removal of the cause caused by external causes. Pulmonary fibrosis is a disease of the respiratory system. In addition to the fibrosis of interstitial diseases of the lung itself, pulmonary fibrosis can be formed due to damage to the lung interstitium by dis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/64B01J27/128
Inventor 强建华施维
Owner BEIJING KAWIN TECH SHARE HLDG
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