One-pot sequential palladium-catalyzed defluorinative amination and Nazarov cyclization for the diastereoselective synthesis of α-fluorinated naphthocyclopentanones.

A one-pot protocol combining Pd-catalyzed defluorinative amination and TfOH‑promoted Nazarov cyclization enables diastereoselective synthesis of α‑fluorinated naphthocyclopentanones from α,α‑difluoro ketones and secondary amines. The mild tandem reaction tolerates diverse substrates, giving products in up to 90% yield and >20 : 1 dr for most cases.