Synthesis of β-Arylethenesulfonyl Fluoride via Pd-Catalyzed Nondirected C-H Alkenylation.

A rapid synthesis of β-arylethenesulfonyl fluorides is realized using ligand-accelerated Pd(II)-catalyzed nondirected C-H alkenylation of simple arenes. The newly developed electron-deficient 2-pyridone ligand is crucial for this transformation with arenes as limiting reagent. This protocol features a broad substrate scope and good functional group tolerance. Late-stage functionalization of various pharmaceuticals and their further click manipulations demonstrate this procedure to be highly valuable.