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.