A mild and selective photocatalytic C-H 18F-fluorination reaction has been developed that provides direct access to 18F-fluorinated amino acids. The biodis-tribution and uptake of three 18F-labelled leucine ana-logues via LAT1 mediated transport in several cancer cell lines is reported. PET imaging of mice bearing PC3 (pros-tate) or U87 (glioma) xenografts using 5-[18F]-fluoro-homoleucine showed high tumor uptake and excellent tumor visualization, highlighting the utility of this strat-egy for rapid tracer discovery for oncology
