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revised on 10.08.2020 and posted on 11.08.2020by Qinheng Zheng, Hongtao Xu, Hua Wang, Wen-Ge Han Du, Nan Wang, Huan Xiong, Yuang Gu, Louis Noodleman, Guang Yang, K. Barry Sharpless, Peng Wu
The lack of simple, efficient [18F]fluorination processes and new target-specific organofluorine probes remains the major challenge of fluorine-18-based positron emission tomography (PET). We report here a fast isotopic
exchange method for the radiosynthesis of aryl [18F]fluorosulfate
based PET agents enabled by the emerging sulfur fluoride exchange (SuFEx) click chemistry. The
method has been applied to the fully-automated 18F-radiolabeling of
twenty-five structurally diverse aryl fluorosulfates with excellent
radiochemical yield (83–100%) and high molar activity (up to 281 GBq µmol–1)
at room temperature in 30 seconds. The purification of radiotracers requires no
time-consuming high-performance liquid chromatography (HPLC), but rather a
simple cartridge filtration. The utility of aryl [18F]fluorosulfate is demonstrated by the in vivo tumor imaging by targeting poly(ADP-ribose) polymerase 1 (PARP1).