Step‐Economical Synthesis of Tetrahydroquinolines by Asymmetric Relay Catalytic Friedländer Condensation/Transfer Hydrogenation

Two steps in one reaction: The title relay reaction relies on a combination of an achiral Lewis acid and a chiral Brønsted acid (B*-H in the scheme). This one-pot method provides access to tetrahydroquinoline derivatives with multiple continuous stereogenic centers in high stereoselectivity (>20:1 d.r., 98 % ee).