A ruthenium-catalyzed oxidative coupling of 2-aryl-quinazolinones with olefins via C–H bond activation followed by an intramolecular aza-Michael reaction is described. This strategy allows the direct and efficient construction of pyrrolo[2,1-b]quinazolin-9(1H)-one scaffolds.
![Graphical abstract: Ruthenium-catalyzed oxidative coupling of 2-aryl-4-quinazolinones with olefins: synthesis of pyrrolo[2,1-b]quinazolin-9(1H)-one motifs](http://hg.y866.cn/compound/lib/scimg/usr/1/C5OB00601E.jpg)