Synthesis of Pyridobenzazepines Using a One-Pot Rh/Pd-Catalyzed Process

In recent years, our group has been developing multicatalytic reactions for the synthesis of biologically relevant heterocyclic compounds. An efficient dual-metal catalyzed reaction of electron-deficient <i>o</i>-chlorovinylpyridines with <i>o</i>-aminophenylboronic esters to access pyridobenzazepines is described. Combining a Rh^I-catalyzed arylation followed by a Pd⁰-catalyzed C–N coupling, in a one-pot procedure, provides a simplified method to access heterocycles without workup and purification after each step. The substrate scope encompasses a variety of <i>N</i>-H and <i>N</i>-alkylated pyridobenzazepine variants with yields up to 93%