Development of 18F-Labeled hydrophilic trans-cyclooctene as a bioorthogonal tool for PET probe construction

Muyun Xu; Xinrui Ma; Jessica E. Pigga; He Zhang; Shuli Wang; Weiling Zhao; Huaifu Deng; Anna M. Wu; Rihe Liu; Zhanhong Wu; Joseph M. Fox; Zibo Li

doi:10.1039/D3CC04212J

Development of ¹⁸F-Labeled hydrophilic trans-cyclooctene as a bioorthogonal tool for PET probe construction†

Muyun Xu,

‡^a Xinrui Ma,

‡^a Jessica E. Pigga,‡^b He Zhang,^a Shuli Wang,^a Weiling Zhao,^a Huaifu Deng,^a Anna M. Wu,^c Rihe Liu,^d Zhanhong Wu,*^a Joseph M. Fox

*^b and Zibo Li

*^a

Author affiliations

* Corresponding authors

^a Department of Radiology, Biomedical Research Imaging Center, and Lineberger Comprehensive Cancer Center, the University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
E-mail: zhanhong_wu@med.unc.edu, ziboli@med.unc.edu

^b Department of Chemistry, the University of Delaware, Newark, Delaware, USA
E-mail: jmfox@udel.edu

^c Department of Molecular Imaging and Therapy, Beckman Research Institute, City of Hope, Duarte, California, USA

^d Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA

Abstract

We report the development of a hydrophilic ¹⁸F-labeled a-TCO derivative [¹⁸F]3 (log P = 0.28) through a readily available precursor and a single-step radiofluorination reaction (RCY up to 52%). We demonstrated that [¹⁸F]3 can be used to construct not only multiple small molecule/peptide-based PET agents, but protein/diabody-based imaging probes in parallel.

Chemical Communications

Development of ¹⁸F-Labeled hydrophilic trans-cyclooctene as a bioorthogonal tool for PET probe construction†

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Development of ¹⁸F-Labeled hydrophilic trans-cyclooctene as a bioorthogonal tool for PET probe construction

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