Synthesis of Geminal Difluorides by Oxidative Desulfurization-Difluorination of Alkyl Aryl Thioethers with Halonium Electrophiles in the Presence of Fluorinating Reagents and Its Application for F-18-Radiolabeling

[摘要]：Various omega-substituted 1,1-difluoroalkanes are synthesized in good yields from alkyl aryl thioethers by a new oxidative desulfurization-difluorination protocol with the reagents combination of 1,3-dibromo-5,5-dimethylhydantoin (DBH) as an oxidizer and pyridine .9HF (Py .9HF) as a fluoride source. The reaction proceeds via a fluoro-Pummerer-type rearrangement followed by an oxidative desulfurization-fluorination step. Starting from alpha-fluorinated thioethers, this reaction is promising for F-18-labeling (tau(1/2) = 110 min) of ligands applicable for. positron emission tomography (PET). Using the combination of DBH and carrier-added Py . 9H[F-18]F, an F-18-labeled difluoride was synthesized from the corresponding a-fluoro thioether with a radiochemical yield of 9%.

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