Synthesis of 4-styrylquinazolines enabled by a hypervalent iodine-promoted oxidative amination cascade

<h2>ABSTRACT</h2> Efficient synthetic routes to pharmaceutically important 4-styrylquinazolines scaffolds are of considerable interest. Herein, we report a concise synthesis of 4-styrylquinazoline derivatives <i>via</i> a hypervalent iodine-promoted oxidative amination cascade. Readily available <i>N</i>-(2-acetophenyl)acetamides and benzylamines are employed, with the latter acting as both carbon and nitrogen donors, enabling simultaneous formation of the quinazoline core and the exocyclic alkene. This operationally simple and atom-economical strategy provides a streamlined alternative to conventional stepwise approaches.