METHOD OF PRODUCING N-{5-[3-(THIOPHENE-2-CARBONYL)-PYRAZOLE[1,5-a]PYRIMIDIN-7-YL]-2-FLUORO-PHENYL}-N-METHYL-ACETAMIDE IN POLYMORPHIC MODIFICATION B Russian patent published in 2010 - IPC C07D487/04 A61K31/519 A61P25/08 A61P25/20 

Abstract RU 2404984 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a method for synthesis of N-(5-[3-(thiophene-2-carbonyl)-pyrazole[1,5-a]pyrimidin-7-yl]-2-fluoro-phenyl}-N-methyl-acetamide in polymorphic modification B, in which (5-amino-1H-pyrazol-4-yl)-thiophen-2-yl-methanone reacts with N-[5-(3-dimethylamino-acryloyl)-2-fluoro-phenyl]-N-methyl-acetamide in a solvent selected from a group comprising acetic acid, propionic acid and methanoic acid at 50°C until boiling point of the mixture is reached. (C1-C4)-alcohol is then added to the obtained mixture at temperature of 40°C-80°C, after which the obtained mixture is kept for at least 30 minutes a temperature of 30°C- 55°C for initiating crystallisation. The crystalline product is then separated.

EFFECT: method of obtaining a compound in polymorphic modification B, which can be used in medicine in treating and preventing anxiety, epilepsy, sleep disorders and insomnia.

8 cl, 3 dwg, 1 tbl, 1 ex

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RU 2 404 984 C1

Authors

Anglada Luis

Gul'Etta Antonio

Palomer Al'Bert

Dates

2010-11-27Published

2007-10-10Filed