Crystalline Agomelatine solvate and preparation method thereof

Abstract

The invention discloses a crystalline Agomelatine ethylene glycol, acetic acid solvate and a preparation method thereof. The preparation method of the crystalline Agomelatine ethylene glycol solvate comprises the steps of: mixing Agomelatine with ethylene glycol according to the proportion of 1:2-5, heating the mixture to 100 to 130 DEG C, and melting and cooling the heated mixture to result in solids. The preparation method of the crystalline Agomelatine ethylene glycol solvate further comprises the steps of: dissolving Agomelatine in acetic acid to result in solution, and adding the solution into antisolvent, followed by standing still or constantly stirring or evaporating the solvent below 50 DEG C to result in crystal. The crystalline Agomelatine ethylene glycol, acetic acid solvate prepared according to the method has the advantages of: obviously reduced melting point of the solvate, high crystallization purity, good reproducibility, less amount of the solvent used, no need of protection from inert gas, low production cost, simple operation, mild reaction condition and easy control.

Description

technical field [0001] The invention relates to two crystal forms of agomelatine solvate and a preparation method thereof. Background technique [0002] Agomelatine (agomelatine), the chemical name is N-[2-(7-methoxy-1-naphthyl) ethyl] acetamide, and its trade name is Valdoxan, which is the first estrogen developed by Servier. The melanotropic antidepressant was approved for marketing in the European Union in February 2009. It can effectively treat depression, improve sleep parameters and not affect sexual function. [0003] Agomelatine has dual properties, on the one hand it is an agonist of the melatonin receptor and on the other hand it is a 5-HT 2C receptor antagonists. 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 due to jet lag, appetite disorders and obesity, etc. . [0004] The prepar...

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Problems solved by technology

[0010] Patent CN200610108395.2 The method for preparing agomelatine crystal form has harsh conditions and cannot be popularized and used in industrial production

Patent CN200610108394.8 method to prepare crystal form IV agomelatine needs to be rapidly cooled to 50-70°C and maintained at 70°C for 5 hours, the method has poor reproducibility, and it is easy to produce agomelatine mixed with crystal form III

Patent CN200910160307.7 The preparation of crystal form V agomelatine by spray drying method requires the introduction of inert gas, high production cost and cumbersome operation

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