tert-Butyl peroxybenzoate (TBPB)-mediated copper-catalyzed C(sp3)-H methylation of 4-thiazolidinone

A novel efficient and straightforward protocol for copper-catalyzed direct methylation utilizing peroxides through C(sp3)-H bond activation has been developed. This synthetic method provides methylated 4-thiazolidinones with moderate to good yields under standard optimal conditions. In order to improve the sustainability and usefulness of this transformation, this approach stands out for its affordable copper catalyst, one-pot synthesis, easily accessible methylation reagents, wide range of substrates, and remarkable functional group compatibility. This innovative technique provides a valuable tool for the synthesis of methylated thiazolidinone derivatives and potentially boosting their utility in the development of bioactive building blocks.