Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Reexamination Certificate
2006-02-07
2006-02-07
Bernhardt, Emily (Department: 1624)
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
Reexamination Certificate
active
06995264
ABSTRACT:
The present invention provides a process for preparing aripiprazole in a high purity and a high yield. According to the process of the present invention, aripiprazole is prepared by the reaction of a carbostyril compound represented by general formula (2):(wherein X is halogen atom, lower alkanesulfonyloxy group, arylsulfonyloxy group or an aralkylsulfonyloxy group), with a piperazine compound represented by formula (3):and/or a salt thereof in water, in the presence of 0.5 to 10 mol of an inorganic basic compound, per mol of the carbostyril compound (2).
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Banno, K. et al., “Studies on 2(1H)-Quinolinone Derivatives as Neuroleptic Agents. I. Synthesis and Biological Activities of (4-Phenyl-1-Piperazinyl)-Propoxy-2(1H)-Quinolinone Derivatives”, Chemical and Pharmaceutical Bulletin, Pharmaceutical Society of Japan, Tokyo, Japan, vol. 36, No. 11, pp. 4377-4388, (1988).
Morita, S. et al., “Practical Application of the Palladium-Catalyzed Amination in Phenylpiperazine Synthesis: An Efficient Synthesis of a Metabolite of the Antipsycotic Agent Aripiprazole”, Tetrahedron, Elsevier Science Publishers, Amsterdam, Netherlands, vol. 54, No. 19, pp. 4811-4818, (1998).
Tsujimori Hisayuki
Yamaguchi Tatsuya
Bernhardt Emily
Finnegan Henderson Farabow Garrett & Dunner L.L.P.
Otsuka Pharmaceutical Co. Ltd.
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