Automated Synthesis of NET-Targeted PET Tracers [ 18 F]4F-mHPG and [ 18 F]3F-pHPG through Photocatalyzed 18 F-Deoxyfluorination

作者：Yarong Cao, Yang Xie, Lili Pan, Yueqi Wang, Honghai Yin, Mingxing Hu, Xiaoai Wu, Wei Chen · 发表于：The Journal of Organic Chemistry · 年份：2025 · DOI：10.1021/acs.joc.5c02276 · 被引用次数：4 · 研究领域：Nanoplatforms for cancer theranostics、Cancer, Hypoxia, and Metabolism、Medical Imaging Techniques and Applications

The NET-targeted radiotracers [ 18 F]4F-mHPG and [ 18 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 18 F-deoxyfluorination. [ 18 F]4F-mHPG and [ 18 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.