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Conjugation of radiofluorinated prosthetic groups to primary amines of peptides in an aqueous medium is still considerably challenging. Herein, we report a one-pot cascade synthesis of 1-[F]fluoro-4-isothiocyanatobenzene ([F]), an isothiocyanate-functionalized prosthetic group for radiolabeling of various peptides in aqueous medium. The developed compound [F] was synthesized in >99% radiochemical purity with 22.

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