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Preparation method of agomelatine crystal form A

A single crystal form technology, applied in the field of agomelatine crystal form A preparation, can solve the problems of agomelatine product loss, cumbersomeness, poor reproducibility, etc., and achieves simple and easy operation, difficulty and cost of the method. The effect of reducing and improving the yield

Inactive Publication Date: 2010-07-21
ZHEJIANG HUAHAI PHARMA CO LTD
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  • Summary
  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The preparation methods of agomelatine crystal form mentioned above are somewhat cumbersome. For example, heating and melting agomelatine, and then cooling to obtain the crystal product of the corresponding form requires the use of specific equipment; some reproducibility is not good, and there are uncertain factors For example, crystal form A, crystal form VI and their mixed crystals can be obtained by crystallization with isopropyl ether; some solvent recrystallization methods will cause agomelatine product loss, which greatly increases the difficulty and cost of industrial mass production

Method used

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  • Preparation method of agomelatine crystal form A
  • Preparation method of agomelatine crystal form A
  • Preparation method of agomelatine crystal form A

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Add 100 g of agomelatine and 300 ml of methanol into the reaction flask, heat and stir to dissolve. Cool the obtained agomelatine methanol solution to 10-20°C, slowly add 2400ml of drinking water dropwise, and keep the temperature at 10-20°C; after the dropwise addition, filter the precipitated crystals and dry them in vacuum to obtain agomelatine crystals Form A 99.1 g, yield: 99.1%.

[0027] Gained agomelatine crystal form A product is measured by D / max-rA target X-ray diffractometer (copper to cathode), and is measured by interplanar spacing d, Bragg 2θ angle and relative intensity (with respect to the strongest ray Expressed as a percentage) is expressed as follows:

[0028]

[0029]

[0030] Implementation column 2

[0031] Add 100 g of agomelatine and 500 ml of methanol into the reaction flask, heat and stir to dissolve. Cool the obtained agomelatine methanol solution to 10-20°C, slowly add 5000ml of drinking water dropwise, and keep the temperature at 10...

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Abstract

The invention provides a preparation method of agomelatine crystal form A which has a single endothermic peak at about 100 DEG C under the differential scanning calorimetry.

Description

technical field [0001] The invention relates to a preparation method of crystal form A of agomelatine, an antidepressant drug. Background technique [0002] Agomelatine has a structural formula as shown in formula (I), and its chemical name is N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide. [0003] [0004] Agomelatine is a melatonin 1, 2 (MT1, MT2) receptor agonist and also a 5-hydroxytryptamine 2c (5HT2C) receptor antagonist, which can directly bind to the 5-HT2C receptor of the post-synaptic membrane , so as to exert its antidepressant effect without increasing the concentration of 5-HT in the synapse, so there is no common side effect of 5-hydroxytryptamine reuptake inhibitor drugs and 5-hydroxytryptamine norepinephrine reuptake inhibitor drugs. Another unique target of the drug is the MT receptor. By stimulating the MT1 and MT2 receptors, it can adjust the patient's 24-hour rhythm and improve the patient's sleep quality, thereby promoting the improvement of the overall...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/18C07C231/00
Inventor 周世伟蹇锋
Owner ZHEJIANG HUAHAI PHARMA CO LTD
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