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阿立哌唑的合成
引用本文:朱航昌,陈国华,张军忍,李强.阿立哌唑的合成[J].中国药物化学杂志,2006,16(2):108-109.
作者姓名:朱航昌  陈国华  张军忍  李强
作者单位:中国药科大学,药物化学教研室,江苏,南京,210009
摘    要:以间氨基苯甲醚为原料,经缩合、傅克酰化、成醚、取代4步制得抗精神病药阿立哌唑,并对原工艺进行改进。目标物的化学结构经红外光谱、核磁共振氢谱及质谱确证,该合成方法原料易得,操作简便,总收率为45·1%。

关 键 词:药物化学  药物制备  工艺改进  阿立哌唑
文章编号:1005-0108(2006)02-0108-02
收稿时间:2005-09-19
修稿时间:2005年9月19日

Synthesis of aripiprazole
ZHU Hang-chang,CHEN Guo-hua,ZHANG Jun-ren,LI-Qiang.Synthesis of aripiprazole[J].Chinese Journal of Medicinal Chemistry,2006,16(2):108-109.
Authors:ZHU Hang-chang  CHEN Guo-hua  ZHANG Jun-ren  LI-Qiang
Institution:Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 21009, China
Abstract:Aripiprazole was synthesized by condensation of 7 -( 4-bromobutoxy)-3,4-dihydrocarbostyril(5) and 1-(2,3-dichlor olphenyl)-piper azine dihydrochloride.Compound 5 was prepared by condensation of 7-hydroxy-3,4 -dihydrocarbostyril(4) and 1,4-dibromobutane.Compound 4 was obtained from m-a nisidine by condensation and F-C acylation.The structure of target com pound was confirmed by IR,~1H-NMR,MS and the total yield was 45.1% .This procedure has advantages of simple starting material and convenient operat ions.
Keywords:medicinal chemistry  drug preparation  process improv ement  aripiprazole
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