~(18)F-Fluorination of Unactivated C-H Bonds in Branched Aliphatic Amino Acids: Direct Synthesis of Oncological Positron Emission Tomography Imaging Agents

摘要

A mild and selective photocatalytic C-H ~(18)F-fluorination reaction has been developed that provides direct access to ~(18)F-fluorinated amino acids. The biodistribution and uptake of three ~(18)F-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-[~(18)F]-fluorohomoleucine showed high tumor uptake and excellent tumor visualization, high-lighting the utility of this strategy for rapid tracer discovery for oncology.