Direct β-C(sp ³ )–H Functionalization to Carbonyls: A Route to Aldehydic Acid Derivatives

We describe a general strategy for C═O bond formation through palladium-catalyzed β-C(sp 3 )–H functionalization using sulfoximine as a neutral directing group. This method enables chemoselective oxidation of inert β-C(sp 3 )–H bonds to aldehydes with 2-nitro-iodylbenzene as an exclusive oxidant and oxygen source. The cooperative effect of the directing group and ligand ensures high selectivity. This strategy exhibits broad functional group tolerance and can be used to advance complex molecule development.