METHOD FOR PREPARING (3-CYANO-1H-INDOLE-7-YL)-[4-(4-FLUOROPHENETHYL)-PIPERAZINE-1-YL]METHANONE AND ITS SALTS Russian patent published in 2007 - IPC C07D209/30 C07D209/42 A61K31/404 A61K31/495

Abstract RU 2295519 C2

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for synthesis of a novel (3-cyano-1H-indole-7-yl)-[4-(4-fluorophenethyl)-piperazine-1-yl]methanone of the formula (I): or its physiologically acceptable salts. Method involves (1) the formylation reaction of indole ester of the formula (II): wherein R means (C₁-C₆)-alkyl, and (2) ester formyl of the formula (III): wherein R mean as given above and synthesized at stage (1) is interacted with hydroxylamine to yield an oxime derivative of the formula (IV): wherein R means as given above; (3) oxime of the formula (IV) is converted to cyanoindole ester of the formula (V): wherein R is given above; (4) ester of the formula (V) is saponified to yield 3-cyano-1H-indole-7-carboxylic acid; (5) 3-cyano-1H-indole-7-carboxylic acid is interacted with 1-[2-(4-fluorophenyl)ethyl]-piperazine or its salts to yield compound of the formula (I), and (6) synthesized base of the formula (I) is converted to one of its physiologically acceptable salts by treatment with acid.

EFFECT: improved method of synthesis.

11 cl

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RU 2 295 519 C2

Authors

Krass'E Ehlen

Ehkkert Uve

Bettkher Khenning

Bateh Andreas

Ehmmert Shteffen

Dates

2007-03-20—Published

2001-12-21—Filed