Enantioselective Synthesis of Optically Pure β-Amino Ketones and γ-Aryl Amines by Rh-Catalyzed Asymmetric Hydrogenation

Abstract

A series of optically pure β-amino ketones have been synthesized in high enantioselectivities (ee > 99%) by Rh-DuanPhos-catalyzed asymmetric hydrogenation of readily prepared β-keto enamides. Further reduction of these β-amino ketones with hydrogen and Pd/C leads to the formation of a variety of protected enantiomerically pure γ-aryl amines (ee > 99%), which are key building blocks in many bioactive molecules.