Divergent C–H Alkylation and Allylation of Indoles with Unactivated Alkene via Mechanochemical Rh(III) Catalysis
Abstract
A tunable mechanochemical platform is reported for Rh(III)-catalyzed C2-alkylation (via electrophilic C–H activation) or C2-allylation (via CMD) of indoles with unactivated alkenes, controlled simply by fine-tuning the reagent composition. 1,1-Disubstituted alkenes undergo Rh-free Ag-catalyzed C3-branched alkylation, enabling one-pot synthesis of N -free indoles via tandem coupling–deprotection. The protocol offers broad substrate scope, high yields and selectivity, scalability, and applicability to late-stage drug modification, providing a sustainable and efficient route to valuable indole derivatives.
Fields of Study & Subjects
Crystallography and molecular interactions
Catalytic C–H Functionalization Methods
Axial and Atropisomeric Chirality Synthesis
Publication details
- Journal / source
- Organic Letters
- Publisher
- American Chemical Society (ACS)
- Volume
- 28
- Issue
- 3
- Pages
- 935–941
- Publication date
- 7 January 2026
- Language
- EN