[18F]SuFEx Click Chemistry Enabled Ultrafast Late-stage Radiosynthesis

11 August 2020, Version 2
This content is a preprint and has not undergone peer review at the time of posting.


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).


Click Chemistry
Sulfur Fluoride Exchange
PET Imaging
Late Stage Fluorination
Aryl Fluorosulfate

Supplementary materials

Zheng et al 18SuFEx SI 20200810


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