ChemRxiv
These are preliminary reports that have not been peer-reviewed. They should not be regarded as conclusive, guide clinical practice/health-related behavior, or be reported in news media as established information. For more information, please see our FAQs.
1/1
0/0

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

preprint
revised on 10.08.2020 and posted on 11.08.2020 by 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).

Funding

Sulfur(VI) Fluoride Exchange (SuFEx): new developments and biological applications

National Institute of General Medical Sciences

Find out more...

Chemical Tools for Studying Fucosylated Glycans

National Institute of General Medical Sciences

Find out more...

Quantum Chemistry of Proton Pumping by Cytochrome c Oxidases

National Institute of General Medical Sciences

Find out more...

Sulfur(VI) Fluoride Exchange (SuFEx) Click Chemistry in Macromolecule Synthesis and Fabrication

Directorate for Mathematical & Physical Sciences

Find out more...

History

Email Address of Submitting Author

qhzheng@scripps.edu

Institution

The Scripps Research Institute

Country

United States of America

ORCID For Submitting Author

0000-0002-8440-8673

Declaration of Conflict of Interest

The authors declare no competing financial interest.

Exports