Synthesis of triazolo- and tetrazolo-fused 1,4-benzodiazepines via one-pot Ugi-azide and Cu-free click reactions.

A one-pot Ugi-azide reaction followed by intramolecular Cu-free azide-alkyne cycloaddition generates a polycyclic scaffold 7 bearing polycyclic triazole, tetrazole, and benzodiazepine rings. This method could be extended for obtaining a more complicated scaffold 8 containing a piperazinone ring.