Synthesis of Axially Chiral Amino Acid and Amino Alcohols via Additive−Ligand-Free Pd-Catalyzed Domino Coupling Reaction and Subsequent Transformations of the Product Amidoaza[5]helicene

Novel optically active axially chiral amino acid and amino alcohols have been synthesized efficiently via lactam ring-opening, with the aid of an optically active alcohol, amidoaza[5]helicene 5, which has been readily prepared by an additive-ligand-free Pd catalyzed domino coupling reaction in a single step. The stereostructures of these chiral molecules have also been clarified.