Process for the preparation of carbostyril derivatives

Details Process for the preparation of carbostyril derivatives Process for the preparation of carbostyril derivatives

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) C07D 471/08 (2006.01) C07D 471/10 (2006.01) C07D 487/10 (2006.01)

Patent

CA 2428237

A process for preparing carbostyril derivatives such as aripiprazole is described. Dichlorophenylpiperazine or an acid addition salt thereof is reacted with a compound of formula X-C4H8-Y or X-C4H6-Y to produce a novel quaternary spiro ammonium salt intermediate which is optionally isolated and purified. The quaternary spiro ammonium salt intermediate is reacted with 7- hydroxydihydrocarboxystyryl to produce the carbostyril derivative.

Un procédé de préparation de dérivés de carbostyrile comme l'aripiprazole est divulgué. La dichlorophénylpipérazine ou un sel d'addition acide de cette substance est amené à réagir avec un composé de formule X-C4H8-Y ou X-C4H6-Y pour donner un nouveau spirosel d'ammonium quaternaire comme produit intermédiaire, qui est optionnellement isolé et purifié. On fait réagir cet intermédiaire avec le 7-hydroxydihydrocarboxystyryke pour produire le dérivé de carbostyrile.

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