Abstract.The present review shows metal‐catalyzed oxidative C(sp3)‐H/C(sp2)‐H bond functionalization of 1,4‐benzoxazinones by utilizing various substrates such as indoles, phosphites or phosphine oxides, malonate esters, and resorcinol, which lead to the formation of new C‐C or C‐P bonds.
The metal catalysts used for these couplings include Fe, Cu, Ag, and Ru. This follows a strategy involving either the one‐electron oxidation process (OEO), ball milling technique, or photocatalytic process. The synthesized products in this method show usefulness in natural products, materials, agriculture, and medicinal chemistry.