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 language | English |
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Pages (from-to) | 6660 –6666 |
Number of pages | 7 |
Journal | Angewandte Chemie - International Edition |
Volume | 60 |
Issue number | 12 |
DOIs | |
Publication status | Published - 15 Mar 2021 |
Keywords
- C-H functionalization
- mechanochemistry
- methylation
- organometallics
- late-stage functionalization