Rapid and Atom-Economical <i>De Novo</i> Access to Polysubstituted Quinolines via Sequential C–C Bond Cleavage and Reassembly

Herein, we report a Cu(II), Rh(III) relay-catalyzed multicomponent reaction of easily available arylformylacetonitriles and alkynes, enabling the efficient de novo synthesis of polysubstituted quinolines via two steps in a “one-pot” manner. Various polysubstituted quinolines could be provided in up to 88% yields for 23 examples. The title products exhibit favorable fluorescence emission. Mechanistic studies suggest that unique domino two-C–C bond cleavage and the formation of multiple new bonds (five C–C bonds and one C–N bond) are involved in this process. This protocol features mild reaction conditions and is extremely simple and scalable. The luminescence of the products enhances their promising applications in functional materials.