Enantioselective [4 + 2] Cycloaddition Reaction of Vinylquinolines with Dienals Enabled by Synergistic Organocatalysis

An unprecedented organocatalytic enantioselective [4 + 2] cycloaddition reaction of vinyl quinolines with dienals is achieved with the synergistic activation of CH₃SO₃H and a chiral aminocatalyst. The power of the process is demonstrated by its high efficiency of the production of new synthetically and biologically valued chiral quinoline architectures in high yields and with excellent enantioselectivities.