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Keywords:

  • aryl bromides;
  • halogen exchange;
  • imaging agents;
  • nickel;
  • radioiodination
Thumbnail image of graphical abstract

Rapid and efficient radioiodination of aryl and heteroaryl bromides has been achieved using a nickel(0)-mediated halogen-exchange reaction. This transformation gives direct access to [123I]- and [125I]-imaging agents for single photon emission computed tomography (SPECT), such as 5-[123I]-A85380 (see scheme, Boc=tert-butyloxycarbonyl, cod=1,5-cyclooctadiene, TFA=trifluoroacetic acid).