Synfacts 2025; 21(06): 582
DOI: 10.1055/a-2588-2266
Metals in Synthesis

Broadening Arene C–H Alkylations via Radical−Radical Cross-Coupling

Authors

Großkopf J, Gopatta C, Martin RT, Haseloer A, MacMillan DWC. Princeton University, USA
Generalizing Arene C–H Alkylations by Radical–Radical Cross-Coupling.

Nature 2025;
641: 112-121
DOI: 10.1038/s41586-025-08887-2
 

Significance

This work introduces a powerful and general strategy for late-stage C(sp 2)−H alkylation via selective coupling of differently hybridized radical species, enabling modular scaffold diversification using simple acids and alcohols. It overcomes key limitations of traditional methods and expands access to complex chemical space.


Comment

A sequential radical–radical cross-coupling strategy enables late-stage orthogonal functionalization of drug scaffolds with precision. Leveraging dynamic orbital selection, this method expands chemical space and streamlines the synthesis of complex bioactive molecules.




Publication History

Article published online:
22 May 2025

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