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Sulfur [18F]Fluoride Exchange Click Chemistry Enabled Ultrafast Late-Stage Radiosynthesis.


ABSTRACT: The lack of efficient [18F]fluorination processes and target-specific organofluorine chemotypes remains the major challenge of fluorine-18 positron emission tomography (PET). We report here an ultrafast isotopic exchange method for the radiosynthesis of novel PET agent aryl [18F]fluorosulfate enabled by the emerging sulfur fluoride exchange (SuFEx) click chemistry. The method has been applied to the fully automated 18F-radiolabeling of 25 structurally and functionally diverse aryl fluorosulfates with excellent radiochemical yield (83-100%, median 98%) and high molar activity (280 GBq μmol-1) at room temperature in 30 s. The purification of radiotracers requires no time-consuming HPLC but rather a simple cartridge filtration. We further demonstrate the imaging application of a rationally designed poly(ADP-ribose) polymerase 1 (PARP1)-targeting aryl [18F]fluorosulfate by probing subcutaneous tumors in vivo.

SUBMITTER: Zheng Q 

PROVIDER: S-EPMC8418205 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature

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Sulfur [<sup>18</sup>F]Fluoride Exchange Click Chemistry Enabled Ultrafast Late-Stage Radiosynthesis.

Zheng Qinheng Q   Xu Hongtao H   Wang Hua H   Du Wen-Ge Han WH   Wang Nan N   Xiong Huan H   Gu Yuang Y   Noodleman Louis L   Sharpless K Barry KB   Yang Guang G   Wu Peng P  

Journal of the American Chemical Society 20210225 10


The lack of efficient [<sup>18</sup>F]fluorination processes and target-specific organofluorine chemotypes remains the major challenge of fluorine-18 positron emission tomography (PET). We report here an ultrafast isotopic exchange method for the radiosynthesis of novel PET agent aryl [<sup>18</sup>F]fluorosulfate enabled by the emerging sulfur fluoride exchange (SuFEx) click chemistry. The method has been applied to the fully automated <sup>18</sup>F-radiolabeling of 25 structurally and functio  ...[more]

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