药物中间体N-(5-氟-2苯氧基苯基)乙酰胺的合成

Synthesis of N-(5-Fluoro-2-phenoxyphenyl)acetamide as Drug Intermediate

1,4-二氟-2硝基苯与苯酚在碳酸钾的作用下醚化得到1-(4-氟-2-硝基苯氧基)苯,后者经硝基还原和乙酰化反应合成N-(5-氟-2苯氧基苯基)乙酰胺。并考察了醚化以及乙酰化等关键步骤的反应条件,较佳的反应条件:醚化反应以碳酸钾作为缚酸剂;乙酰化化以三乙胺作为缚酸剂。三步总收率67.2%,产物及中间体经过^(1)H NMR和MS确认。

First,1-(4-fluoro-2-nitrophenoxy)benzene was synthesized from 1,4-difluoro-2-nitrobenzene and phenol by the etherification reaction under the action of potassium carbonate.Then,N-(5-fluoro-2-phenoxyphenyl)acetamide was synthesized by nitro reduction and acetylation reaction.The reaction conditions of etherification and acetylation reactions were investigated.The optimum synthetic condition was given as follows:in the etherification reaction,potassium carbonate was used as acid binding agent;in the acetylation reaction,triethylamine was used as acid binding agent.The overall yield of the final product was 67.2%.The target compound was determined by 1H-NMR and MS.