Recent Advances and Prospects in the Amination of Benzoxazoles

Abstract Aminoheterocycles are important class of heterocycles and many of the natural products and drug molecules are observed as the derivatives of aminoheterocycles. Consequently, their efficient synthetic protocols have gained more attention among organic chemists. Benzoxazole is one of the familiar fused heterocyclic compounds showing vibrant biological activities, and is seen as the backbone in various biologically important compounds and drugs. The new C−N bond construction on benzoxazole by the coupling between sp 2 carbon at the 2‐position of benzoxazole and nitrogen from several nitrogen sources enhanced their properties, and the area of amination of benzoxazole is relatively rich in literature. In this review, we have compiled the recent advances in the amination of benzoxazoles by giving an overview and covering literature up to 2021.