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Novel intermediates useful for the preparation of aripiprazole and methods for the preparation of the novel intermediates and aripiprazole
Novel intermediates useful for the preparation of aripiprazole and methods for the preparation of the novel intermediates and aripiprazole
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机译:可用于制备阿立哌唑的新型中间体以及制备该新型中间体和阿立哌唑的方法
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摘要
The invention disclosed in this application relates to an improved process for thepreparation 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 inthe 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 inventionalso relates to the novel intermediates of the formulae (2) & (3) and processesfor their preparation.
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