C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 215/22 (2006.01) C07C 49/67 (2006.01) C07D 295/088 (2006.01)
Patent
CA 2584789
The invention disclosed in this application relates to an improved process for the preparation of aripiprazole (1) which comprises (i) Reacting 6-hydroxy-l- indanone (11) with 1,4-dihalobutane (12) in the presence of a base and a solvent at a temperature in the range of 90 to 110 deg C to form the novel intermediate 6-(4-halo butoxy)-indan-l-one (3), (ii) reacting the novel intermediate with 1-(2,3-clichlorophenyl)-piperazine (9) to get another novel intermediate 6-[4-[4-(2,3-dichlorophenyl)-l-piperazinyl] butoxy]-indan-l-one (2) and (iii) Reacting the resulting novel compound with sodium azide. The invention also relates to the novel intermediates of the formulae (2) & (3) and processes for their preparation.
L~invention décrite dans la présente demande concerne un procédé amélioré de préparation de l~aripiprazole (1), selon lequel : (i) on fait réagir de la 6-hydroxy-1-indanone (11) avec du 1,4-dihalobutane (12) en présence d~une base et d~un solvant, à une température allant de 90 à 110 degrés C, afin de former le nouvel intermédiaire 6-(4-halobutoxy)indan-1-one (3) ; (ii) on fait réagir le nouvel intermédiaire avec de la 1-(2,3-dichlorophényl)pipérazine (9) pour obtenir un autre nouvel intermédiaire 6-[4-[4-(2,3-dichlorophényl)-1-pipérazinyl] butoxy]indan-1-one (2) ; et (iii) on fait réagir le nouveau composé résultant avec de l~azide sodique. L~invention concerne également les nouveaux intermédiaires de formules (2) et (3) et des procédés pour les préparer.
Arava Veera Reddy
Athukuru Venkata Subba Rao
Chinnapillai Rajendiran
Jasti Venkateswarlu
Cassan Maclean
Suven Life Sciences Limited
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