Ir-catalyzed reductive amination and transfer hydrogenation of diketones: access to β- and γ-amino alcohols

Abstract

β- and γ-Amino alcohols are among the most significant structural motifs in pharmacologically active molecules and pharmaceuticals. Herein, a protocol for the construction of β- and γ-amino alcohols via reductive amination and transfer hydrogenation of diketones with aromatic amines is described. This reaction is performed by utilizing iridium complexes as catalysts and HCO₂H as a hydrogen donor to deliver a library of β- and γ-amino alcohols under mild and operationally simple conditions. Successful scale-up performance was also conducted under standard conditions.