3-氯-4-(3-氟苄氧基)苯胺的合成

    Practical Synthesis of 3-Chloro-4-(3-fluorobenzyloxy) aniline

    • 摘要: 目的 开发一条适合产业化的3-氯-4-(3-氟苄氧基)苯胺的合成工艺路线。方法 以间氟氯苄和2-氯-4-硝基苯酚为原料,依次经碳酸钾存在下的缩合反应、铁粉/氯化铵还原得到3-氯-4-(3-氟苄氧基)苯胺。结果 总收率为82%。所得产物经TLC、熔点和核磁共振氢谱表征,具有高纯度。结论 本方法原料价廉易得,操作简便,环境污染更小,预期适合工业化生产。

       

      Abstract: OBJECTIVE To develop a practical process for 3-chloro-4-(3-fluorobenzyloxy)aniline. METHODS 3-Chloro- 4-(3-fluorobenzyloxy)aniline was synthesized from 1-(chloromethyl)-3-fluorobenzene and 2-chloro-4-nitrophenol via condensation in the presence of potassium carbonate, followed by reduction with Fe/NH4Cl. RESULTS The overall yield of this process was 82%. The target product was characterized by TLC, melting point and 1H-NMR. CONCLUSION This synthetic process features are cheap and readily available starting materials, robustness, less waste burden, thus should be amenable to industrial production.

       

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