1.
Angew Chem Int Ed Engl
; 60(12): 6660-6666, 2021 Mar 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-33031646
RESUMO
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.