• Journal of Radiopharmaceuticals and Molecular Probes
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• v.10 no.1
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• pp.51-62
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• 2024

Boron neutron capture therapy (BNCT) stands at the forefront of cancer treatment, offering a pioneering approach to enhance the rate of recovery for patients who show noncompliance to conventional therapies. The ¹⁸F labeling of BNCT tracers signifies a groundbreaking leap in molecular imaging. Hence, the aim of this brief review is to outline the radiofluorination strategies utilized for BNCT tracers. Radiofluorination of L-BPA, a ligand of L-type amino acids, can be carried out via electrophilic as well as nucleophilic substitution reactions. It's solubility can be elevated by complexing it with fructose to form BPA-fructose complex, followed by radiolabeling with ¹⁸F. In addition to electrophilic and nucleophilic radiofluorination, we have briefly presented the radiofluoro exchange method, which is applicable for amino acids having trifluoroborate groups, i.e., FBY (fluoroboronotyrosine), featuring both imaging and therapeutic functionalities. Furthermore, this review offers an inclusive array of radiofluorination strategies employed for other BNCT tracers, including o-carborane and fenbufen boronopinacol.