A highly enantioselective four-component reaction for the efficient construction of chiral β-hydroxy-α-amino acid derivatives

An enantioselective four-component reaction of a diazoketone, water, an aniline and ethyl glyoxylate in the presence of catalytic Rh₂(OAc)₄ and a chiral Brønsted acid was developed to efficiently produce β-hydroxy-α-amino acid derivatives in good yields with high diastereoselectivity and enantioselectivity.