Automated Synthesis of NET-Targeted PET Tracers [ <sup>18</sup> F]4F-mHPG and [ <sup>18</sup> F]3F-pHPG through Photocatalyzed <sup>18</sup> F-Deoxyfluorination
The NET-targeted radiotracers [<sup>18</sup>F]4F-mHPG and [<sup>18</sup>F]3F-pHPG have demonstrated promising clinical applications; however, the preparation of these tracers remains challenging. Herein, we report an improved synthesis protocol that enables the efficient automated production of two PET tracers via photocatalyzed <sup>18</sup>F-deoxyfluorination. [<sup>18</sup>F]4F-mHPG and [<sup>18</sup>F]3F-pHPG were prepared in excellent n.d.c. RCYs of 31.3 ± 0.4% and 22.4 ± 1% in only 1 h from readily available precursors, and further validated on the PC12 tumor model for head-to-head comparison.
Authors
- Lili Pan (ORCID: https://orcid.org/0000-0003-3903-071X)
- Xiaoai Wu (ORCID: https://orcid.org/0000-0002-3518-9689)
- Honghai Yin
- Yarong Cao
- Wei Chen (ORCID: https://orcid.org/0000-0002-3694-5204)
- Yueqi Wang (ORCID: https://orcid.org/0000-0002-0374-1045)
- Yang Xie
- Mingxing Hu
Institutions
- China National Nuclear Corporation (CN)
- Sichuan University (CN)
- West China Hospital of Sichuan University (CN)
- Sichuan University of Science and Engineering (CN)
Publication Details
- Journal
- The Journal of Organic Chemistry
- Published
- 2025-12-05
- DOI
- https://doi.org/10.1021/acs.joc.5c02276
- Citations
- 3
- Primary Topic
- Nanoplatforms for cancer theranostics
- Type
- article
- Field-Weighted Citation Impact
- 2.02