Radiosynthesis of [18f]arylscf2h using aryl boronic acids, s-(chlorofluoromethyl) benzenesulfonothioate and [18f]fluoride

Abstract

Herein, we report a mild and practical protocol for the copper-catalyzed chlorofluoromethylthiolation of (hetero)aryl boronic acids with the novel reagent PhSO2SCFClH. The resulting products are amenable to halogen-exchange 18F-fluorination with cyclotronproduced [18F]fluoride affording [18F]ArSCF2H. This process highlights the combined value of reagent development and (hetero)aryl boron precursors for radiochemistry by adding the [18F]SCF2H group to the list of 18F-motifs within reach for positron emission tomography studies.