Palladium-Catalyzed Asymmetric Three-Component Reaction between Glyoxylic Acid, Sulfonamides and Arylboronic Acids for the Synthesis of alpha-Arylglycine Derivatives

14 February 2023, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


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.


asymmetric catalysis
amino acids
multicomponent reaction
Petasis reaction
boronic acids

Supplementary materials

Supporting Information
Experimental procedures, analytical data and copies of NMR spectra and HPLC chromatograms


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