Preparation method of 2-(7-methoxy-1-naphthyl) acetonitrile

A methoxyl and naphthyl technology, applied in a new preparation field, can solve the problems of harsh reaction requirements, environmental pollution, incomplete reaction, etc., and achieve the effects of mild reaction conditions, high product purity, and short reaction route
CN102336686AInactive Publication Date: 2012-02-01SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Publication Date
2012-02-01
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a new preparation method of an important intermediate of the antidepressant agomelatine, i.e. 2-(7-methoxy-1-naphthyl) acetonitrile. In the method, a compound of formula III is subjected to a Wittig reaction so as to obtain a compound of formula XI, which then undergoes an aromatization reaction, so that 2-(7-methoxy-1-naphthyl) acetonitrile can be obtained. The preparation method of the invention has a short reaction route, the Wittig reaction and the aromatization reaction both have high yield. With mild reaction conditions and without anything to do with reagents and solvents etc. of high toxicity, the preparation method provided in the invention is suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a new preparation method of an important intermediate of agomelatine, 2-(7-methoxy-1-naphthyl)acetocyanide. Background technique

[0002] On February 24, 2009, agomelatine, the world's first melatonin receptor agonist antidepressant, was approved for marketing in the European Union. Agomelatine was developed by the French company Servier. , whose trade name is Valdoxan / Thymanax, is currently approved by the European Union for the treatment of depression in adults. Its chemical name is N-[2-(7-methoxyl-1-naphthyl)ethyl]acetamide, trade name Valdoxan, and its structural formula is as shown in formula II below:

[0003]

[0004] The launch of agomelatine is a new breakthrough in the field of depression treatment. Its innovation lies in its unique mechanism of action: it is the world's first melatonin (MT 1 , MT 2 ) receptor agonist, but also five serotonin 2c (5H...

Claims

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