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Abstract

This protocol describes a procedure for the synthesis of α, β-branched-b-amino aldehydes via Proline-catalyzed asymmetric Mannich reaction of aldehydes with N-tert–butoxycarbonyl-imines. The crystalline β-amino aldehydes are formed in good yields and extremely high levels of diastereo- and enantioselectivities without the need for chromatographic purification and are readily oxidized to the corresponding β-amino acids. The protocol can be completed in approximately 14 h on small scales or up to 30 h on larger scales.