Maleimides as Versatile Reactive Platforms in Transition‐Metal‐Catalyzed C–H Activation/Annulation

ABSTRACT Maleimide‐containing molecules serve as important scaffolds for biological activities as well as photochemical properties and play a significant role in both the academic and industrial communities. Maleimides are versatile coupling partners owing to their diverse reactivities with transition‐metal catalysts in C–H activation and annulation reactions including alkenylation, alkylation, fused‐annulation, and spiro‐annulation for the synthesis of numerous maleimide‐containing bioactive molecules such as succinamides, lactams, and lactims. In this review, innovative advances toward the synthesis of biologically important maleimide/succinimide‐bearing scaffolds through C–H activation and annulation reactions with transition metal as catalysts, with particular emphasis on the intermediates, transition states, and incorporation of different annulation sites for maleimide is reviewed. This review covers research published between 2019 and 2025, highlighting the substrate scope, reaction mechanisms, synthetic transformations, and future prospects of this approach.