An endo‐Directing‐Group Strategy Unlocks Enantioselective (3+1+2) Carbonylative Cycloadditions of Aminocyclopropanes

Abstract An endo ‐directing group strategy enables enantioselective (3+1+2) cycloadditions that are triggered by carbonylative C−C bond activation of cyclopropanes. These processes are rare examples of cycloadditions where C−C bond oxidative addition is enantiodetermining, and the first where this is achieved within the context of a multicomponent (higher order) reaction design.