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One-Pot Synthesis of 2-Substituted 4-Aryl-4,5-dihydro-3,1-benzoxazepines from 2-(2-Aminophenyl)-1-arylethanols via Dehydration of the Corresponding Amides

  作者 Fukamachi, S; Konishi, H; Kobayashi, K  
  选自 期刊  Helvetica Chimica Acta;  卷期  2011年94-6;  页码  987-992  
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[摘要]An efficient method for the preparation of 2-substituted 4-aryl-4,5-dihydro-3,1-benzoxazepine derivatives under mild conditions has been developed. The reaction of 2-(2-aminophenyl)ethanols 1 with acid chlorides in the presence of excess Et3N in THF at room temperature gave the corresponding N-acylated intermediates 2, which were dehydrated by treatment with POCl3 to give 2-substituted 4-aryl-4,5-dihydro-3,1-benzoxazepines 3 in a one-pot reaction.

 
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