Simple and effective method for high-selectivity removal of alpha-monomethyl of 2,6-dimethyl-4-pyridone derivative

A technology for pyridone and derivatives, which is applied in the field of removing α-monomethyl of 2,6-dimethyl-4-pyridone derivatives, can solve the problem of yield less than 5%, high reaction temperature and excessive strong base The use of strong acid and other problems can achieve the effect of good catalytic effect, few experimental steps and easy operation.
CN102977013BInactive Publication Date: 2014-08-27HENAN NORMAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HENAN NORMAL UNIV
Publication Date
2014-08-27
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a simple and effective method for high-selectivity removal of an alpha-monomethyl of a 2,6-dimethyl-4-pyridone derivative. The simple and effective method comprises that an alpha-monomethyl of a 2,6-dimethyl-4-pyridone derivative is removed by oxygen as an oxidizing agent in the presence of anhydrous ferric chloride as a catalyst with heating; and after the reaction, cooling, extraction and separation processes are carried out so that a 6-methyl pyridone derivative is obtained simply and has a high yield. The simple and effective method has the advantages that there is only a reaction step; a flow is simple; the raw materials and the catalyst are cheap and easily available chemical materials; and a reaction organic solvent can be recovered easily and be recycled so that a reaction process is clean and efficient and large-scale industrial production can be realized.
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Description

technical field

[0001] The invention relates to a method for removing α-monomethyl of 2,6-dimethyl-4-pyridone derivatives, specifically using oxygen as an oxidant and anhydrous ferric chloride as a catalyst, and using DMSO as a solvent A method for removing a methyl group at the α-position of a 2,6-dimethyl-4-pyridone derivative. The method has the advantages of environmental friendliness, good compatibility of important functional groups, and good regioselectivity. Background technique

[0002] 4-Pyridone derivatives have diverse biological activities and are widely used in chemical and chemical fields such as medicine and pesticides. In the pharmaceutical industry, it can be used to produce the anti-atherosclerotic drug Xuemaining. It can also be used to produce the broad-spectrum anthelmintic drug Qupinujing which is effective against roundworms, fasciola brucei, whipworms and pinworms. As well as cortisone acetate, hydrocortisone, niacin, ashbelin, and more. 2,6-luti...

Claims

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