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Mechanochemical Solvent‐Free Catalytic C−H Methylation
Author(s) -
Ni Shengjun,
Hribersek Matic,
Baddigam Swarna K.,
Ingner Fredric J. L.,
Orthaber Andreas,
Gates Paul J.,
Pilarski Lukasz T.
Publication year - 2021
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.202010202
Subject(s) - methylation , regioselectivity , catalysis , chemistry , rhodium , compatibility (geochemistry) , combinatorial chemistry , solvent , organic chemistry , materials science , biochemistry , gene , composite material
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.