Sun, YangCramer, Nicolai2019-01-032019-01-032019-01-032018-11-1910.1002/anie.201810887https://infoscience.epfl.ch/handle/20.500.14299/153301WOS:000453344500042Sulfoximines with stereogenic sulfur atoms are attractive structural motifs in drug discovery. A direct catalytic enantioselective method for the synthesis of sulfur-chiral 1,2-benzothiazines from readily accessible diaryl sulfoximines is presented. Rhodium(III) complexes equipped with chiral cyclopentadienyl ligands and paired with suitable carboxylic acid additives engage in an enantiodetermining C-H activation directed by the sulfoximine group. Subsequent trapping of the rhodacycle with a broad range of diazoketones gives access to S-chiral 1,2-benzothiazines with synthetically highly attractive substitution patterns in good yields and enantioselectivities.Chemistry, MultidisciplinaryChemistryasymmetric catalysisc-h activationchiral cyclopentadienyl ligandsrhodiumsulfoximinescatalyzed asymmetric-synthesiskinetic resolutionkinase inhibitornitrene transferligandsactivationc(sp(2))-hsulfidesacidshydroarylationtext::journal::journal article::research article