Cu()-catalyzed C6-selective C-H thiolation of 2-pyridones using air as the oxidant

The Cu( ii )-catalyzed and chelate-directed C6-selective C-H thiolation of 2-pyridones with disulfides was developed to provide aryl and alkyl thioethers. This transformation uses a catalytic amount of Cu(OAc) 2 and molecular oxygen in air as an oxidant, no cocatalysts or metallic oxidants are required. The reaction accommodated both electronic and steric factors at the C3-C5 positions of 2-pyridones, which is efficient for the C6 thiolation of a broad range of 2-pyridones with up to 93% yield. Cu(II)-catalyzed C6-selective C-H thiolation of 2-pyridones with aryl and alkyl disulfides to provide functional thioethers has been achieved.