A One-Pot Three-Step Cu-Catalyzed Protocol to Construct Dibenzo[1,4]diazepine Derivatives and Their Analogs with...

ortho-Substituted primary arylamines are significant functional compounds and important basic building blocks to construct dibenzo[1,4]diazepine derivatives and their analogs. Here, we reported a method for an efficient Cu-catalyzed synthesis of ortho-substituted primary arylamines using cyclopropylamine as the ammonia surrogate in 61∼92% isolated yields and subsequently a one-pot three-step Cu-catalyzed protocol to afford dibenzo[1,4]diazepine derivatives and their analogs in 52∼81% total isolated yields. Further, three key intermediates of dibenzo[1,4]azepine drugs were synthesized on a gram-scale.