| Literature DB >> 33630577 |
Qinheng Zheng1, Hongtao Xu2, Hua Wang1,3, Wen-Ge Han Du4, Nan Wang2, Huan Xiong2, Yuang Gu2, Louis Noodleman4, K Barry Sharpless1, Guang Yang2, Peng Wu3.
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.Entities:
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Year: 2021 PMID： 33630577 PMCID： PMC8418205 DOI： 10.1021/jacs.0c09306
Source DB: PubMed Journal: J Am Chem Soc ISSN： 0002-7863 Impact factor: 15.419