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2-(4-溴甲基苯基)丙酸合成
引用本文:刘志雄,程清蓉,章爱华. 2-(4-溴甲基苯基)丙酸合成[J]. 精细化工中间体, 2008, 38(6)
作者姓名:刘志雄  程清蓉  章爱华
作者单位:1. 吉首大学,化工学院,湖南,吉首,416000
2. 武汉工程大学,化学与制药学院,湖北,武汉,430074
摘    要:以甲苯为原料,经Friedel-Crafts、Willgerodt-Kindler-水解"一锅法",单甲基化和溴代反应合成了洛索洛芬的关键中间体2-(4-溴甲基苯基)丙酸。结果表明:超声波能促进Friedel-Crafts、Willgerodt-Kindler水解反应,使用复合相转移催化剂可得高收率的单基化产物。该合成路线操作简便、原料易得,总收率55.1%。

关 键 词:2-(4-溴甲基苯基)丙酸  傅克反应  Willgerodt-Kindler法  单甲基化  溴代

Synthesis of 2-(4-Bromomethylphenyl)propionic Acid
LIU Zhi-xiong,CHENG Qing-rong,ZHANG Ai-hua. Synthesis of 2-(4-Bromomethylphenyl)propionic Acid[J]. Fine Chemical Intermediates, 2008, 38(6)
Authors:LIU Zhi-xiong  CHENG Qing-rong  ZHANG Ai-hua
Affiliation:LIU Zhi-xiong1,CHENG Qing-rong2,ZHANG Ai-hua1 (1. College of Chemistry , Chemical Engineering,Jishou University,Jishou 416000,China,2. School of Chemical Engneering , Pharmacy,Wuhan Institute of Chemical Technology,Wuhan 430073,China)
Abstract:2-(4-Bromomethylphenyl)propionic acid which was a key intermediate of loxoprofen was synthesized from toluene through four reaction steps including Friedel-Crafts reaction, Willgerodt-Kindler-hydrolysis, monomethylation and bromination. The results showed that the reaction process of Friedel-Crafts and Willgerodt-Kindler-hydrolysis was promoted via ultrasonic, high-yield of ɑ-monomethylation product was obtained by complex phase transfer catalysisis, and overall yield was 55.1% , indicating that this was an efficient synthetic route with convenient operations and available reagents.
Keywords:2-(4-bromomethylphenyl)propionic acid   Friedel-Crafts   Willgerodt-Kindler   ɑ -monomethylation   bromination
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