Efficient Construction of Polycyclic Derivatives via a Highly Selective CuI-Catalyzed Domino Reductive-Aldol Cyclization

A versatile methodology for the diastereo- and enantioselective domino reductive-aldol cyclizations is reported. By using a copper (I)/diphosphane ligand, various five- and six-membered rings were generated with good to excellent diastereo- and enantioselectivities (cis:trans up to 100:0 and ee up to 95%).