An efficient Pd-catalyzed selective C (sp3)-H acetoxylation of 8-methylquinazolinones was reported. Due to the versatility of organic acetates, the route provides facile access to various C8-acetoxylated quinazolinones. The approach is significant because of its features like mild reaction conditions, decent tolerance of functional groups, and wide substrate scope. The monoselective acetoxylation established here may find significant claims in the area of C–H activation.