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Preparing method for agomelatine drug for curing depressive disorder

A compound and reaction technology, which is applied in the field of preparation of agomelatine, a drug for treating depression, can solve problems such as industrialization difficulties, incomplete aromatization, and difficulty in obtaining purified products

Inactive Publication Date: 2013-04-03
LIAONING BENYUAN PHARMACY CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The industrialization of this method is difficult, and the aromatization of the obtained intermediate (7-methoxy-3,4-dihydro-1(2H)-naphthalenyl)ethyl acetate is often incomplete, and it is difficult to obtain a purified product

Method used

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  • Preparing method for agomelatine drug for curing depressive disorder

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Embodiment Construction

[0028] The following examples are intended to illustrate the present invention in detail, but not to limit the present invention.

[0029] Preparation of Methoxyacenaphthylquinone

[0030] In the reactor, add 6.33g (0.04mol) of 2-naphthyl methyl ether and 200ml of dry dichloroethane, cool down to -10°C, add 250ml of oxalyl chloride dropwise, and then add anhydrous trichloride in batches at -10°C Aluminum 10.67 (0.08mol), after the addition, keep stirring at -10-0°C for 8.5 hours, then naturally raise the temperature to ambient temperature and stir overnight, pour the reaction solution into cold hydrochloric acid aqueous solution under stirring, and separate the organic phase, the aqueous phase was extracted with dichloroethane, the organic phases were combined, dried over anhydrous sodium sulfate, the solvent was evaporated under reduced pressure, and the residue was recrystallized with dioxane to obtain 7.47g, with a yield of 88%.

[0031] Preparation of (7-methoxy-1-naphthy...

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Abstract

The invention relates to an N-[2-(7-methoxyl-1-naphthyl) ethyl] acetamide (compound 1) and a preparing method for an intermediate thereof. The compound 1-agomelatine is another drug of vital importance for curing mental diseases, and is the first melatonin receptor stimulant and a 5-hydroxytryptamine2C (S-HTx) receptor antagonist. Animal experiments and clinical research show that the drug has the effects of anti-depression, anti-anxiety, sleep rhythm adjustment and internal clock adjustment, has few untoward effects, brings no influence on sexual function, and adopts the following structure (refer to the specification).

Description

technical field [0001] The present invention relates to the preparation method of N-[2-(7-methoxynaphthalene-1-yl)ethyl]acetamide (compound 1) and its intermediates. Background technique [0002] Agomelatine was developed by Servier and first launched in Europe in 2009. Agomelatine is the first melatonin receptor agonist with good antidepressant effect. Its onset of action is fast, and it has a good curative effect on depression and its accompanying symptoms such as anxiety and insomnia, with few adverse reactions and high safety. [0003] The listing 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 1 , 2 (MT 1 MT 2 ) receptor agonist, but also five serotonin 2c (5HT2c) receptor antagonist. The mechanism of action of agomelatine is completely different from the commonly used antidepressant drugs "selective serotonin reuptake inhibitor (SSRI) and seroton...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/18C07C231/02C07C59/64C07C51/377
Inventor 陈家骏李昕昊王艳胡忠涛田雪孙龙
Owner LIAONING BENYUAN PHARMACY CO LTD
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