Copper-Mediated Direct and Selective C-H Thiolation of Quinazolinones

Direct thiolation of quinazolinones by selective cleavage of a relatively inert C-H bond, mediated by earth-abundant copper and guided by a pyridine or pyrimidine moiety, has been achieved under operationally simple conditions. The devised protocol does not require any toxic or reactive reagents and provides direct access to a broad spectrum of pharmaceutically relevant thioquinazolinones.