Process for preparing aripiprazole

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 215/22 (2006.01)

Patent

CA 2555289

The invention encompasses the synthesis of aripiprazole from BBQ and DCP, and comprises mixing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril (BBQ) and 1-(2,3~- dichlorophenyl)piperazine hydrochloride (DCP) in the presence of at least one base and at least one organic solvent to form a reaction mixture; heating the reaction mixture for a sufficient amount of time to effect the reaction; and isolating aripiprazole. The invention also encompasses the use of phase transfer catalysts in synthesizing aripiprazole from BBQ and DCP.

L'invention concerne la synthèse d'aripiprazole à partir de BBQ et de DCP : mélange de 7-(4-bromobutoxy)-3,4-dihydrocarbostyril (BBQ) et d'hydrochlorure de 1-(2,3--dichlorophényl)pipérazine (DCP) en présence d'au moins une base et d'au moins un solvant organique pour former un mélange de réaction; échauffement du mélange pendant une durée suffisante pour la conduite de la réaction ; et isolation de l'aripiprazole. L'invention concerne également l'utilisation de catalyseurs de transfert de phase dans la synthèse considérée.

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