Synthesis of [1,2,3]-triazolo[1,5-a][1,4]benzodiazepines via an unprecedented one-pot Cu-catalyzed azidation-cyclization reaction

A novel three-step approach leading to [1,2,3]-triazolo[1,5-a][1,4]benzodiazepines in moderate to good yields has been developed. The key step is an unprecedented one-pot Cu-catalyzed azidation-cyclization reaction of ortho-bromobenzylpropargylamines.