Multicomponent Synthesis of Isoindolinone Frameworks via RhIII‐Catalysed in situ Directing Group‐Assisted Tandem Oxidative Olefination/Michael Addition

Abstract A Rh III ‐catalysed three‐component synthesis of isoindolinone frameworks via direct assembly of benzoyl chlorides, o ‐aminophenols and activated alkenes has been developed. The process involves in situ generation of o ‐aminophenol (OAP)‐based bidentate directing group (DG), Rh III ‐catalysed tandem ortho C−H olefination and subsequent cyclization via aza‐Michael addition. This protocol exhibits good chemoselectivity and functional group tolerance. Computational studies showed that the presence of hydroxyl group on the N ‐aryl ring could enhance the chemoselectivity of the reaction.