Angew. Chem. Int. Ed. 2025, e202422899
DOI: 10.1002/anie.202422899
Li Y.; Liu X.; Sham V.; Logvinenko I.; Xue J.; Wu J.; Fu J. et al.
Incorporating fluorine into aliphatic rings induces significant changes in molecular conformation, acidity/basicity, and lipophilicity. A general method has been developed to transform exocyclic alkenes into saturated F2-rings. This reaction utilizes the reagent C6F5I(OAc)2, enabling the straightforward synthesis of gem-difluorinated macrocyclic, fused, spiro, bridged, and natural product-derived structures. The practicality of this protocol is demonstrated through several decagram-scale syntheses.