PROCESS FOR THE PREPARATION OF BUSPIRONES OF HIGH PURITY AND HYDROCHLORIDES THEREOF

The invention relates to a process for the preparation of 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]butyl}-8-azaspiro[4.5]d ecan e-7,9-dione {buspirone} of the formula and of its hydrochlorides by hydrogenating 8-{4'-[4''-(pyrimidin-2'...

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Hauptverfasser:	LASZLO KONCZ, ILONA SZTRUHAR, MARGIT CSORGO, KLARA REITER NEE ESSES, GYULA SIMIG, KALMAN NAGY, EVA FURDYGA, TIBOR MEZEI, ZOLTAN BUDAI, JUDIT SZEGO, ATTILA MANDI, GABOR BLASKO, IMRE KLEBOVICH, GYOGYI VERECZEKEY NEE DONATH
Format:	Patent
Sprache:	eng
Schlagworte:	APPARATUS THEREFOR CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOIDCHEMISTRY CHEMISTRY GENERAL METHODS OF ORGANIC CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PERFORMING OPERATIONS PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS THEIR RELEVANT APPARATUS TRANSPORTING
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Beschreibung
Zusammenfassung:	The invention relates to a process for the preparation of 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]butyl}-8-azaspiro[4.5]d ecan e-7,9-dione {buspirone} of the formula and of its hydrochlorides by hydrogenating 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]but-2'-ynyl}-8-azaspiro [4.5 ]decane-7,9-dione of the formula in the presence of a palladium or Raney nickel catalyst in an organic solvent and optionally converting the 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]butyl}-8-azaspiro[4.5]d ecan e-7,9-dione into a hydrochloride, in which a solution of 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]but-2'-ynyl}-8-azaspiro [4.5 ]decane-7,9-dione of the formula II in an organic solvent whose concentration is at least 40% by weight is added to a suspension of the catalyst in an organic solvent, the catalyst is removed and a) the 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]butyl}-8-azaspiro[4.5]d ecan e-7,9-dione base of the formula I is isolated and/or b) the 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]butyl}-8-azaspiro[4.5]d ecan e-7,9-dione base of the formula I is treated with hydrogen chloride at 15 to 40 DEG C in ethanol or isopropanol and the 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]butyl}-8-azaspiro[4.5]d ecan e-7,9-dione hydrochloride melting at 188 to 191 DEG C is isolated or c) the 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]butyl}-8-azaspiro[4.5]d ecan e-7,9-dione base of the formula I is treated at at most 70 DEG C with hydrogen chloride in ethyl acetate or isopropanol and the 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]butyl}-8-azaspiro[4.5]d ecan e-7,9-dione hydrochloride melting at 201 to 203 DEG C is isolated.