An Efficient Nickel‐Catalyzed Asymmetric Oxazole‐Forming Ugi‐Type Reaction for the Synthesis of Chiral Aryl‐Substituted THIQ Rings

Abstract A nickel‐catalyzed asymmetric oxazole‐forming Ugi reaction of C,N‐cyclic azomethine imines and isonitriles is disclosed. The reported protocol proceeds smoothly, and gives the corresponding adducts, which contain two important pharmaceutically active ring‐systems (tetrahydroquinoline and oxazole rings), in good yields and excellent enantioselectivities by employing an easily accessible chiral diamine as a ligand. This simple and efficient strategy provides easy access to a series of C1‐substituted aryl tetrahydroisoquinolines.