A mild and selective photocatalytic C-H ¹⁸F-fluorination reaction has been developed that provides direct access to ¹⁸F-fluorinated amino acids. The biodistribution and uptake of three ¹⁸F-labeled leucine analogues via LAT1 mediated transport in several cancer cell lines is reported. Positron emission tomography imaging of mice bearing PC3 (prostate) or U87 (glioma) xenografts using 5-[¹⁸F]-fluorohomoleucine showed high tumor uptake and excellent tumor visualization, highlighting the utility of this strategy for rapid tracer discovery for oncology.
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Nodwell et al. (2017) studied this question.
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