METHOD OF PREPARATION HIGH CLEAR BUSPIRON AND ITS HYDROCHLORIDE

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

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Hauptverfasser:	SZEGO JUDIT, CSORGO MARGIT, VERECZKEY GYONGYI NEE DONATH, BLASKO GABOR, FURDYGA EVA, MANDI ATTILA, MEZEI TIBOR, KONCZ LASZLO, KLEBOVICH IMRE, BUDAI ZOLTAN, NAGY KALMAN, SIMIG GYULA, REITER NEE ESSES KLARA, SZTRUHAR ILONA
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]decane-7,9-dione {buspirone} of the formula (I) and of its hydrochlorides by hydrogenating 8-{4'-[4''- -(pyrimidin-2'''-yl)piperazin-1''-yl]but-2'-ynyl}-8-aza- -spiro[4.5]decane-7,9-dione of the formula (II) 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]decane-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]decane-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]decane-7,9-dione base of the formula (I) is treated with hydrogen chloride at 15 to 40 C in ethanol or isopropanol and the 8-{4'-[4''-(pyrimidin-2'''-yl)piperazin-1''-yl]butyl}- -8-azaspiro[4.5]decane-7,9-dione hydrochloride melting at 188 to 191 C is isolated or c) the 8-{4'-[4''-(pyrimidin-2'''- -yl)piperazin-1''-yl butyl}-8-azaspiro[4.5]decane-7,9-dione base of the formula (I) is treated at at most 70 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]decane-7,9-dione hydrochloride melting at 201 to 203 C is isolated.