2-甲基-1-取代苯基-2-丙胺类化合物的简便制备方法  

An Efficient Method for the Synthesis of 2-Methyl-1-substituted-phenyl-2-propylamines

作　　者：朱兰平 赵帅[1] 仓志鹏 周安迪 陈新[1] Zhu Lanping;Zhao Shuai;Cang Zhipeng;Zhou Andi;Chen Xin(School of Pharmaceutical Engineering ＆ Life Science,Changzhou University,Changzhou 213164)

机构地区：[1]常州大学制药与生命科学学院,常州213164

出　　处：《有机化学》2018年第7期1695-1702,共8页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21272029)资助项目~~

摘　　要：2-甲基-1-取代苯基-2-丙胺是合成β_2肾上腺素受体激动剂类药物的重要中间体.以取代氯化苄为原料,通过与异丁腈发生烷基化反应,所得产物经过水解,Curtius重排和钯碳催化氢化反应,合成了一系列2-甲基-1-取代苯基-2-丙胺.此方法操作简便安全,原料经济易得,产率较高,可以适用于制备多种类型的2-甲基-1-取代苯基-2-丙胺类化合物.2-Methyl-1-substituted-phenyl-2-propylamines are key intermediates for synthesizing the β2 adrenoceptor agonists. A series of 2-methyl-l-substituted-phenyl-2-propylamines have been synthesized starting from substituted benzyl chlorides. Isobutyronitrile was alkylated with benzyl chloride, and the resulting 2-methyl-l-aryl-2-butylcynide was hydrolyzed to give the corresponding acid. Curtius rearrangement of the acid and catalytic hydrolgenation of the resulting Cbz-protected amine afforded the title compound. The method is simple and safe to operate, the raw materials are readily available and the overall yields are satisfactory. This method is suitable for the synthesis of 2-methyl-2-（2-methylphenyl）-phenyl-2-propylamine and various kinds of derivatives.

关 键 词：2-甲基-1-取代苯基-2-丙胺 Β2肾上腺素受体激动剂 Curtius重排 合成 

分 类 号：O625.63[理学—有机化学] TQ460.1[理学—化学]