Abstract
Biomolecules labeled with radioisotopes of iodine and fluorine play a major role in
science and medicine, with a range of applications including molecular imaging of
disease, as radiopharmaceuticals for therapy and as tools for drug discovery. Due
to the relative stability of Csp2–halogen bonds, radioiodine and radiofluorine labels are commonly incorporated into
tracers via arene substitution. The wide availability of aryl boron reagents has led
to their use for the development of radioiodination and radiofluorination methods,
particularly using transition-metal complexes for accelerated reactions. Here, we
review the range of transition-metal-mediated methods that have been developed for
radiohalogenation of aryl boron compounds. Applications of these transformations for
the preparation of molecular imaging agents and the use of new technologies to advance
automated synthesis or high-throughput discovery are also described.
1 Introduction
2 Radioiodination Using Aryl Boron Reagents
2.1 Applications of Copper-Mediated Radioiodination Reactions
3 Radiofluorination Using Aryl Boron Reagents
3.1 Radiofluorination Using Palladium, Nickel and Silver Complexes
3.2 Radiofluorination Using Copper Complexes
3.3 Applications of Copper-Mediated Radiofluorination Reactions
3.4 New Technology for Copper-Mediated Radiofluorination Reactions
4 Conclusions
Key words
aromatic halogenation - radioiodine - radiofluorine - transition-metal catalysis -
medical imaging
