Mechanochemical Solvent‐Free Catalytic C−H Methylation
Shengjun Ni, Matic Hribersek, Swarna K. Baddigam, Fredric J. L. Ingner, Andreas Orthaber, Paul J. Gates, Lukasz T. Pilarski
Abstract
Abstract The mechanochemical, solvent‐free, highly regioselective, rhodium‐catalyzed C−H methylation of (hetero)arenes is reported. The reaction shows excellent functional‐group compatibility and is demonstrated to work for the late‐stage C−H methylation of biologically active compounds. The method requires no external heating and benefits from considerably shorter reaction times than previous solution‐based C−H methylation protocols. Additionally, the mechanochemical approach is shown to enable the efficient synthesis of organometallic complexes that are difficult to generate conventionally.
Topics & Concepts
MethylationCatalysisRegioselectivityChemistryRhodiumCombinatorial chemistrySolventCompatibility (geochemistry)Organic chemistryMaterials scienceBiochemistryGeneComposite materialCatalytic C–H Functionalization MethodsSynthesis and Catalytic ReactionsCatalytic Cross-Coupling Reactions