Preparation method of high-purity nepafenac intermediate

An intermediate, acetamide technology, applied in the field of pharmaceutical synthesis, can solve the problems of defective refining methods, harsh reaction conditions, low reaction temperature, etc., and achieve the effects of easy control, rapid reaction and high product purity
CN112794809APending Publication Date: 2021-05-14NANJING GRITPHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
NANJING GRITPHARMA CO LTD
Publication Date
2021-05-14

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Abstract

The invention provides a preparation method of a high-purity nepafenac intermediate, which belongs to the technical field of medicine synthesis. The preparation method comprises the following steps of dissolving a chlorinating agent in an organic solvent, reacting with 2-aminobenzophenone at low temperature, carrying out heating reaction on the generated intermediate and 2-(methylthio)acetamide, after the reaction is finished, carrying out post-treatment, separating to obtain a 2-amino-3-benzoyl-alpha-(methylthio)phenylacetamide crude product, and recrystallizing the crude product to obtain a refined product of the 2-amino-3-benzoyl-alpha-(methylthio)phenylacetamide.
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Description

Technical field

[0001] The present invention belongs to the field of drug synthesis, and more particularly to a method of preparing a high-purity nappermine intermediate 2-amino-3-benzoyl-α-(methylthio) phenylthylethylidemide.Background technique

[0002] Naphemine is a novel eye to non-steroidal antipyretic town pain resistant anti-inflammatory drugs. Treatment of inflammation. At present, the results show that Nai Phene is better than traditional non-steroidal antipyretic impections and is good safe. On August 19, 2005, the US Food and Drug Administration allowed its eyes to use the suspension (trade name Nevanac, Alton) to clinically, making it a first ophthalmic anti-hormone precision precursor approved by FDA drug.

[0003] Naphifen amine, chemically called 2-amino-3-benzoyl phenylacetamide, the structural formula is as follows:

[0004]

[0005] In 1981, the preparation method of Naphen is first disclosed in 1981, the patented, the patented patentol, the secondchlorite, tert-butyl hypochlorite...

Claims

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