Divergent Synthesis of β‐Hydroxy Amides (Esters) and γ‐Amino Alcohols via Ir/f‐Diaphos Catalyzed Asymmetric Hydrogenation

Abstract

AbstractThe iridium/f‐diaphos L2 or L9 catalyzed asymmetric hydrogenation of β‐aryl β‐keto amides (esters), and β‐amino ketones to afford two enantiomers of the desired chiral alcohols was realized with 90%‐99% yield and 73%‐99% ee. This protocol could be easily conducted on gram scale in the presence of low catalyst loading (up to 9900 TON). Moreover, the hydrogenated products are versatile building blocks for a variety of biologically active molecules and drugs, such as Fluoxetine, Dapoxetine and so on.magnified image