Atroposelective sp3 C—H Coupling for Kinetic Resolution of Thioanilide Atropisomers

Main observation and conclusion A highly efficient kinetic resolution of racemic thioanilide atropisomers via C(sp 3 )−H arylation has been achieved by a hybrid palladium catalyst bearing an anionic chiral Co III ‐complex and a phosphoramidite ligand, leading to both enantioenriched atropisomeric arylation thioanilides (up to 99% ee) and N‐Me atropisomeric thioanilides (up to 99% ee), simultaneously. The remained enantioenriched substrates can be arylated again by using an achiral anionic ligand to give the enantiomer with the opposite configuration.