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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 disclosure relates to a process for the preparation of aripiprazole (1) which comprises (i) Reacting 6-hydroxy-1-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 intermediate 6-(4-halo butoxy)-indan-1-one (3), (ii) reacting the intermediate (3) of step (i) with 1-(2,3-clichlorophenyl)-piperazine (9) to get another intermediate 6-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl] butoxy]-indan-1-one (2) and (iii) Reacting the resulting compound with sodium azide. The disclosure also relates to the intermediates of the formulae (2) & (3) and processes for their preparation.
机译:本公开涉及一种制备阿立哌唑(1)的方法,该方法包括(i)在碱和溶剂的存在下,使6-羟基-1-茚满酮(11)与1,4-二卤代丁烷(12)反应。温度在90到110摄氏度之间以形成中间体6-(4-卤代丁氧基)-茚满-1-酮(3),(ii)使步骤(i)的中间体(3)与1-( 2,3-三氯苯基)-哌嗪(9)得到另一种中间体6- [4- [4-(4-(2,3-二氯苯基)-1-哌嗪基]丁氧基]-茚满-1-酮(2)和(iii)使所得化合物与叠氮化钠反应。本公开内容还涉及式(2)和(3)的中间体及其制备方法。

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