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Novel intermediates useful for the preparation of aripiprazole and methods for the preparation of the novel intermediates and aripiprazole

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

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.
机译:本申请中公开的发明涉及一种用于制备阿立哌唑(1),其包括(i)使6-羟基-1-茚满酮反应(11)在碱和溶剂的存在下,在1,4-二卤代丁烷(12)中在90至110摄氏度的温度范围内形成新型中间体6-(4-卤代丁氧基)-茚满-1-酮(3),(ii)使新型中间体与1-(2,3-氯氯苯基)-哌嗪(9)反应得到另一种新型中间体6- [4- [4-(4-(2,3-二氯苯基)-1-哌嗪基]丁氧基]-茚满-1-酮(2)和(iii)使所得新化合物与叠氮化钠反应。本发明还涉及式(2)和(3)的新型中间体和方法为他们的准备。

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