Direct 18 F-Fluorosulfurylation of Phenols and Amines Using an [ 18 F]FSO 2 + Transfer Agent Generated In Situ .

We report the direct radiofluorosulfurylation method for the synthesis of 18 F-labeled fluorosulfuryl derivatives from phenols and amines using an [ 18 F]FSO 2 + transfer agent generated in situ . Nucleophilic radiofluorination is achieved even in a hydrous organic medium, obviating the need for azeotropic drying and the use of cryptands. This unprecedented, operationally simple isotopic functionalization facilitates the reliable production of potential radiotracers for positron emission tomography, rendering facile access to SuFEx radiochemistry.