Dual Role of Anthranils as Amination and Transient Directing Group Sources: Synthesis of 2-Acyl Acridines

The transient directing group promoted C(sp2)–H functionalization of benzaldehydes with anthranils by a cationic rhodium(III) catalyst is described. Notably, anthranils have been used as both transient directing groups and amination sources to afford 2-acyl acridines through direct C–H amination followed by acid-mediated cyclization. A range of substrate scopes and functional group tolerance were observed.