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5-methyl-2(1H)pyridone derivatives, and preparation method and application thereof

A technology for pyridone and derivatives, which is applied in the field of 5-methyl-2-pyridone derivatives and its preparation, and can solve the problems of preparation methods and uses of 5-methyl-2(1H) pyridone derivatives, There are no other problems, and the effect of low cost, simple steps and few processes is achieved

Inactive Publication Date: 2015-11-25
SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] At present, there are no reports of 5-methyl-2 (1H) pyridone derivatives shown in formula I of the present invention; there is no preparation of 5-methyl-2 (1H) pyridone derivatives shown in formula I Methods and Uses Reported

Method used

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  • 5-methyl-2(1H)pyridone derivatives, and preparation method and application thereof
  • 5-methyl-2(1H)pyridone derivatives, and preparation method and application thereof
  • 5-methyl-2(1H)pyridone derivatives, and preparation method and application thereof

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Embodiment 1

[0078]

[0079] Among them, "rf" is the abbreviation of reflux, and its Chinese meaning is "reflux".

[0080] In a 25ml reaction bottle, first add 3.4ml from 17mlH 2 O and the solution (50%, volume fraction) that 17ml concentrated sulfuric acid forms, then add 1g (0.01mol) 2-amino-5-picoline, cool to below 10 ℃ with ice-salt bath, after stirring several minutes, reaction solution Turned milky white. Then slowly drop by (1.72gNaNO 2 with 3mlH 2O) the mixed solution, during dropwise addition, produces irritating gas, after dropwise addition, the reaction solution turns into a light yellow solution, and TCL (thin layer chromatography) monitors until the reaction is complete (about 40min). Then add 8mlH 2 O, reflux stirring reaction 15min, cooling, add anhydrous Na under stirring 2 CO 3 , make the reaction solution neutral (produce yellow-brown solid), filter, the gained filtrate is spin-dried, then dissolve and filter with absolute ethanol, and the gained filtrate is spi...

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Abstract

The invention discloses 5-methyl-2(1H)pyridone derivatives disclosed as Formula I, or crystal forms, pharmaceutically acceptable salts, hydrates, solvates or pro-drugs thereof. In the formula I, R is selected from hydroxy group, mercapto group, amino group or imino group. The invention provides the new 5-methyl-2(1H)pyridone derivatives; and the new 5-methyl-2(1H)pyridone derivatives have obvious inhibiting effects on fibroblast proliferation and fibroblast secretory fiber binding protein (Fn), and can be used for preparing drugs for treating or preventing fibrosis diseases, tumors and the like. The preparation method of the compounds disclosed as Formula I has the advantages of fewer procedures, simple steps, mild reaction conditions, low energy consumption, high efficiency, low cost, environment friendliness and the like, and is very suitable for application in industry.

Description

technical field [0001] The invention relates to a 5-methyl-2(1H) pyridone derivative and its preparation method and application. Background technique [0002] 5-Methyl-2(1H)pyridone, alias: 5-methylpyridin-2-ol, 2-hydroxy-5-methylpyridine, CAS number: 1003-68-5, its chemical structure is shown in Formula A It is mainly used in fields such as organic synthesis. [0003] [0004] U.S. Patent No. 3,839,346A discloses pyridone compounds shown in formula B, which have anti-inflammatory, antipyretic, lower serum uric acid levels, and analgesic effects; wherein, the number of substituents R is 0 or 1, and R represents nitro, chlorine, etc. atom, alkyl, methoxy; when R is 0, the compound shown in formula B is 1-phenyl-5-methyl-2-(1H)pyridone (ie pirfenidone). US Patent No. 4,052,509A also discloses pirfenidone, which has good anti-inflammatory and analgesic effects. [0005] [0006] Chinese patent CN1386737A discloses an anti-fibrosis pyridone drug represented by formula C...

Claims

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Application Information

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IPC IPC(8): C07D213/643A61K31/4412A61P35/00A61P11/00A61P17/00A61P1/16A61P31/14A61P37/06A61P13/12A61P9/10
CPCC07D213/643
Inventor 尹述凡黎勇曹婷婷袁丽宋长伟
Owner SICHUAN UNIV
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