Rhodium‐Catalyzed Enantioselective and Diastereoselective Hydrogenation of β‐Ketoenamides: Efficient Access to anti 1,3‐Amino Alcohols

Valuable chiral building blocks were synthesized with excellent enantioselectivity and diastereoselectivity through tandem hydrogenation of (Z)-β-ketoenamides, which were in turn prepared by the direct condensation of 1,3-diketones with acetamide (see scheme). The chiral amino alcohol products can be converted into useful γ-aryl isobutylamines through hydrogenolysis with Pd/C. R1=aryl, heteroaryl, methyl; R2=alkyl.