Palladium-Catalyzed Cross-Coupling of 4-(Tosyloxy)quinazolines with H-Phosphonates and Phosphine Oxides: An Efficient Access to 2-(Hetero)aryl-4-phosphorylated Quinazolines

A series of 2-(hetero)aryl-4-phosphorylated quinazolines was successfully synthesized in moderate to excellent yields via a palladium-catalyzed C-O/P-H cross-coupling reaction of 4-(tosyl-oxy)quinazolines with H-phosphonates and phosphine oxides. This efficient and green methodology provides an alternative straightforward protocol for the introduction of phosphorus groups to quinazoline compounds at the C4 position via C-O activation.

Automated summary

An efficient and green methodology was developed for the synthesis of a series of 2-(hetero)aryl-4-phosphorylated quinazolines via a palladium-catalyzed C-O/P-H cross-coupling reaction, providing an alternative protocol for introducing phosphorus groups to quinazoline compounds at the C4 position through C-O activation.