One‐Pot Synthesis of Chiral 1‐Aryl‐2‐Aminoethanols via Ir‐Catalyzed Asymmetric Hydrogenation

Abstract

AbstractA straightforward synthesis approach to chiral 1‐aryl‐2‐aminoethanols via the one‐pot asymmetric hydrogenation catalyzed by Ir catalyst was developed. This tandem process involves the in situ generation of α‐amino ketones via the nucleophilic substitution of α‐bromoketones with amines and the Ir‐catalyzed asymmetric hydrogenation of ketone intermediates to provide diverse enantiomerically enriched β‐amino alcohols. The excellent yields and enantioselectivities (up to 96 % yield and up to >99 % ee) with a wide substrate scope in this one‐pot strategy were obtained.