Mechanochemical Solvent-Free Catalytic C—H Methylation

Dr. Shengjun Ni, Matic Hribersek, Swarna K Baddigam, Fredric J. L Ingner, Dr. Andreas Orthaber, Paul J Gates, Lukasz T Pilarski*

*Corresponding author for this work

Research output: Contribution to journalArticle (Academic Journal)peer-review

14 Citations (Scopus)
9 Downloads (Pure)

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.
Original languageEnglish
Pages (from-to)6660 –6666
Number of pages7
JournalAngewandte Chemie - International Edition
Volume60
Issue number12
DOIs
Publication statusPublished - 15 Mar 2021

Keywords

  • C-H functionalization
  • mechanochemistry
  • methylation
  • organometallics
  • late-stage functionalization

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