Asymmetric Synthesis of Azepinoindoles via Enantioselective Ugi‐4CR/post‐Ugi Transformation Sequence

Abstract An efficient and convenient protocol for synthesizing enantioenriched azepinoindoles was developed. In the presence of catalytic stereo genic‐at‐cobalt(III) complexes, an enantioselective four component Ugi reaction (Ugi‐4CR) is achieved under mild conditions, delivering chiral Ugi‐adducts with up to 97:3 er, which subsequently underwent an enantiospecific gold‐catalyzed cyclization to access chiral azepinoindole frameworks.