A palladium-catalyzed enantioselective three-component reaction of glyoxylic acid, sulfonamides and aryltrifluoroborates is described. This process provides modular access to the important α-arylglycine motif in moderate to good yields and enantioselectivies. The formed α-arylglycine products constitute useful building blocks for the synthesis of peptides or arylglycine-containing natural products.

A palladium-catalyzed enantioselective three-component reaction of glyoxylic acid, sulfonamides and aryl trifluoroborates is described. This process provides modular access to the important alpha-arylglycine motif in moderate to good yields and enantioselectivies. The formed alpha-arylglycine products constitute useful building blocks for the synthesis of peptides or arylglycine-containing natural products.

A palladium-catalyzed asymmetric three-component synthesis of alpha-arylglycine derivatives starting from glyoxylic acid, sulfonamides and arylboronic acids is reported. This novel, operationally simple method offers access to the alpha-arylglycine scaffold in good yields and enantioselectivities. The utilization of a tailored catalyst system enables the enantioselective synthesis of the desired alpha-arylglycines despite a fast racemic background reaction. The obtained products can be directly employed as building blocks in peptide synthesis.