Oxazinoazaarenes as Versatile Intermediates for Regioselective Late-Stage C–H-Functionalization and Skeletal Editing of Pyridines, Isoquinolines and Quinolines

Abstract

Azaarenes, particularly pyridines, represent some of the most important structural and functional motifs across various fields. Consequently, late-stage C–H bond functionalization and skeletal editing of azaarenes hold significant value, particularly for accelerating structure–activity relationship studies. Dearomatized intermediates derived from such azaarenes offer an innovative strategy for selectively modifying these valuable cores. Among them, oxazinoazaarenes are a practical and scalable platform for regioselective meta- and para-C–H functionalization and skeletal editing of the azaarene moiety. This short review highlights the advancements in oxazinoazaarene-based pyridine modification methods achieved by our group and others.