We report here the latest embodiment of sulfur (VI) fluoride exchange (SuFEx) click chemistry — anionic fluoride exchanges with the fluorine atom of aryl fluorosulfate. We apply a time-dependent saturation transfer (TDST) NMR technique to study the otherwise difficult to detect fluoride exchange process. The process is effective with either [19F] or [18F]fluoride salts at room temperature. The SuFEx method for [18F]-radiolabeling features the rapid rate, clean reaction, mild condition, minimal purification and tolerance for a wide range of functional groups. The ability of aryl [18F]fluorosulfate as a radiotracer for positron-emitting tomography (PET) imaging is demonstrated by a successful in vivo localization study of xenograft tumor tissue by a [18F]-radiolabeled poly ADP ribose polymerase (PARP) targeting small molecule aryl fluorosulfate.

Sulfur [18F]/[19F]fluoride exchange of aryl fluorosulfate: Click chemistry and new agents for PET imaging

2019 Spring National Meeting

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