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Nickel-Mediated Radioiodination of Aryl and Heteroaryl Bromides: Rapid Synthesis of Tracers for SPECT Imaging


  • Financial support from the Scottish Funding Council, SINAPSE, and GE Healthcare is gratefully acknowledged. We would also like to thank M. Beglan and Dr. T. H. Flowers for performing AAS measurements.


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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).