Journal of Jishou University(Natural Sciences Edition)

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Simple Synthesis of Pharmaceutical Intermediates  of β-Halogenated Phenethylamine

YU Jian,LI Zengzeng,JIANG Ting,LEI Qian,SHENG Huixiang,GUAN Mengdan,HOU Kun,YUAN Li,LI Pei,LI Ling,TANG Shi   

  1. (College of Chemistry and Chemical Engineering,Jishou Univcrsity,Jishou 416000,Hunan China)
  • Online:2018-05-25 Published:2018-06-27


A highly efficient and simple method for the synthesis of pharmaceutical intermediates of β-halogenated phenethylamine has been developed.Using ethyl bromoacetate and dibenzylamine as starting material,the desired ethyl 2-acetamido-3-chloro-3-(4-methoxyphenyl)propanoate was synthesized through sequential substitution,addition,catalytic hydrogenation,chlorination and acylation.The strategy provides a convenient way for natural products and pharmaceutical molecules containing multifunctional structural units of ethylamine.The reaction conditions were optimized and the optimum synthetic route was determined.Moreover,the target product was characterized by melting point,H NMR and 3C NMR.

Key words: pharmaceutical intermediates, dibenzylamine, ethyl bromoacetate, substitution, hydrogenation

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