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阿立哌唑的合成
引用本文:陈光勇,陈旭冰,刘光明,邓杰.阿立哌唑的合成[J].大理学院学报,2007,6(8):8-9.
作者姓名:陈光勇  陈旭冰  刘光明  邓杰
作者单位:1. 大理学院药学院,云南大理,671000
2. 重庆医药工业研究院,重庆,400061
摘    要:目的:研究非典型抗精神病药物阿立哌唑的合成路线及工艺.方法:通过优化反应溶剂、反应温度、反应时间及加料方式,以7-羟基-3,4-二氢-2-(1H)-喹啉酮为起始原料,经N-溴丁基化和O-烃基化合成了阿立哌唑.结果:阿立哌唑的结构通过IR、1H-NMR(CDCl3)及13C-NMR(CDCl3)确认.结论:本方法反应条件温和,操作简便,且提高了反应收率.

关 键 词:阿立哌唑  合成  7-羟基-3  4-二氢-2-(1H)-喹啉酮
文章编号:1672-2345(2007)08-0008-02
修稿时间:2007-03-29

Synthesis of aripiprazole
CHEN Guang-yong,CHEN Xu-bing,LIU Guang-ming,DENG Jie.Synthesis of aripiprazole[J].Journal of Dali University,2007,6(8):8-9.
Authors:CHEN Guang-yong  CHEN Xu-bing  LIU Guang-ming  DENG Jie
Institution:1. College of Pharmacy, Dali University, Dali, Yunnan 671000, China;2.Chongqing Pharmaceutical Research Institute , Chongqing 400061, China
Abstract:Objective:To improve the process for the preparation of the atypical antipsychotics aripiprazole.Methods:Starting from 7-hydroxide-3,4-dihydro-2(1H) quinolone,and by optimization of the solvents used,temperature and method of adding materials in each step atypical antipsychotics aripiprazole was synthesized through N-butylation and O-alkylation.Results:Structure of the product was confirmed by IR,1H-NMR(CDCl3)and13C-NMR(CDCl3).Conclusion:This synthetic route had a mild reaction condition and improved yield,and was easily controlled.
Keywords:aripiprazole  synthesis  7-hydroxide-3  4-dihydro-2(1H) quinolone
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