Zhu Yong-cha
2010
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Journal
Chinese Journal of Modern Drug Application
Abstract
Objective To synthesize aripiprazole,a novel antipsychotic drug.Methods aripiprazole was prepared from 1-(2,3-dichlorophenyl)piperazine hydrochloride by condensation with 1,4-dibromobutane followed by reaction with 7-hydroxy-3,4-dihydrocarbostyril.Results The overall yield was 45% aripiprazole was achieved.The process is suitable for industrial producing.the intermediate's structure is 8-(2,3-dichloro-phenyl)-5,8-diaza-spiro[4,5]decane bromide.Conclusion The synthetic method is economical,convenient and suitable for industrial production.It's proved that the intermediate's structure is 8-(2,3-dichloro-phenyl)-5,8-diaza-spiro[4,5]decane bromide and not 1-(4-bromo-butyl)-(2,3-dichloro-phenyl)-piperazine reported in the literature.