A One-Pot Three-Step Cu-Catalyzed Protocol to Construct Dibenzo[1,4]diazepine Derivatives and Their Analogs with Cyclopropylamine as a Surrogate of Ammonia
Abstract
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.
Fields of Study & Subjects
Synthesis and pharmacology of benzodiazepine derivatives
Catalytic C–H Functionalization Methods
Cyclopropane Reaction Mechanisms
Publication details
- Journal / source
- Organic Letters
- Publisher
- American Chemical Society (ACS)
- Volume
- 28
- Issue
- 5
- Pages
- 1634–1638
- Publication date
- 24 January 2026
- Language
- EN