Preparation method of celecoxib

A technology of celecoxib and amides, applied in the field of new celecoxib preparation, can solve the problems of long reaction period, up to 24 hours, difficult to realize industrialization, etc., to achieve excellent product quality, reduce reaction time, avoid The effect of post-processing
CN103570622AActive Publication Date: 2014-02-12北京京卫燕康药物研究所有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
北京京卫燕康药物研究所有限公司
Publication Date
2014-02-12

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Abstract

The invention provides a preparation method of celecoxib. The preparation method provided by the invention can improve the yield and the purity and save the cost by using an amide solvent.
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Description

technical field

[0001] The invention relates to a new preparation method of Celecoxib. Background technique

[0002] As we all know, celecoxib is a new type of non-steroidal anti-inflammatory drug and type II cyclooxyesterase (COX-2) inhibitor developed by Searle Company of the United States. Patent CN94194833.1 first disclosed its structure and anti-inflammatory effect.

[0003] Celecoxib chemical name: 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (CAS: 169590-42- 5)

[0004] The structure of celecoxib is as follows:

[0005]

[0006] Celecoxib can be prepared by the following methods:

[0007]

[0008] Step 1: p-methylacetophenone and ethyl trifluoroacetate in methanol, tetrahydrofuran, methyl tert-butyl ether, isopropanol, or a mixture of these solvents, and react in the presence of a basic compound , to prepare 4,4,4-trifluoro-1-(4-methylphenyl)-1,3-butanedione:

[0009] For example:

[0010] Patent US6232472 describes that i...

Claims

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