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Method for preparing high-purity agomelatine

A high-purity, pure product technology, which is applied in the preparation of carboxylic acid amides, chemical instruments and methods, and the preparation of organic compounds, etc., can solve the problems of environmental pollution and complicated processes, and achieve reduced pollution, high purity, and reduced synthesis steps Effect

Inactive Publication Date: 2014-11-05
郭炳华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] The above-mentioned routes are complicated in technology and pollute the environment, so it is still of great significance to study new synthetic routes, especially the new synthetic routes that are easy to operate and less pollute the environment.

Method used

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  • Method for preparing high-purity agomelatine
  • Method for preparing high-purity agomelatine
  • Method for preparing high-purity agomelatine

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Embodiment 2

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Abstract

The invention relates to preparation of a high-purity antidepressant agomelatine and aims to prepare active pharmaceutical ingredients of the agomelatine simply and in large scale. A method is characterized in that 7-methoxytetrahydronaphthalene-1-one (represented as the formula II) is employed as a starting raw material and is reacted with cyanoacetic acid to prepare a compound represented as the formula (III). The compound represented as the formula (III), with the effect of high-purity manganese dioxide, is subjected to dehydrogenation to obtain a compound represented as the formula (IV). The compound represented as the formula (IV) is subjected to hydrogenation reduction and acetylization to obtain a compound represented as the formula (I). The compound represented as the formula (I) is agomelatine. An agomelatine crude product is subjected to purification to obtain high-purity agomelatine.

Description

technical field [0001] The invention relates to the technical field of a method for industrially producing high-purity agomelatine. Background technique [0002] The chemical name of agomelatine is N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, and its structural formula is shown in the following formula (I). Its trade name is Valdoxan, which is the first melatonin antidepressant developed by Servier in France, and it was launched in Germany and the UK in 2009. It can effectively treat depression, improve sleep parameters and maintain sleep quality. features of sexual function. [0003] [0004] Agomelatine has dual properties. On the one hand, it is an agonist of the melatonin receptor; on the other hand, it is an antagonist of the 5-HT2C receptor. These properties make it central nervous system active, especially in the treatment of major depression, seasonal affective disorder, sleep disorders, cardiovascular conditions, digestive system conditions, insomnia and fatigue...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/18C07C231/02
Inventor 郭炳华
Owner 郭炳华
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