METHOD OF CRYSTALLIZATION OF 1-[2-(2-NAPHTHYL)-ETHYL]-4-(3- TRIFLUOROMETHYLPHENYL)-1,2,3,6-TETRA-HYDROPYRIDINE HYDROCHLORIDE, PREPARED CRYSTALLINE FORMS AND PHARMACEUTICAL COMPOSITION Russian patent published in 2002 - IPC

Abstract RU 2192416 C2

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention describes method of crystallization of 1-[2-(2-naphthyl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetra- hydropyridine hydrochloride (SR 57746A) that involves the following stages: a) indicated compound is dissolved at heating in solvent taken among alkanols having from 1 to 2 carbon atoms, acetone, dimethyl-sulfoxide and ethyl acetate being indicated solvent comprise optionally from 5 to 30% of water or aqueous hydrochloric acid; b) prepared solution is cooled to temperature 0/+10 C at the rate from 3 to 100 C/h at stirring at the rate from 0 to 600 rev/min; c) prepared product is isolated and micronized optionally. Invention describes three forms of (SR 57746A): form I, form II, form III and mixture of form I and form III, and also pharmaceutical composition used for treatment of neurodegeneration comprising compound SR 57746A in optionally micronized crystalline form taken among form I, form II, form III and mixture of form I/form III. EFFECT: improved method of crystallization, valuable medicinal properties, enhanced activity of active component. 24 cl, 4 dwg, 2 tbl, 16 ex

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RU 2 192 416 C2

Authors

Karon Antuan

Frank Brjuno

Monn'E Oliv'E

Dates

2002-11-10Published

1997-12-23Filed