Copper-Mediated Late-Stage Iodination and 123I-Labelling of Triazole-benzimidazole Bioactives

@article{Fjellaksel2018CopperMediatedLI,
  title={Copper-Mediated Late-Stage Iodination and 123I-Labelling of Triazole-benzimidazole Bioactives},
  author={Richard Fjellaksel and R. Sundset and P. Riss and J{\o}rn H Hansen},
  journal={Synlett},
  year={2018},
  volume={29},
  pages={1491-1495}
}
The copper-mediated azide-alkyne cycloaddition has been studied to achieve late-stage introduction of iodine onto novel triazole-benzimidazole Gonadotropin Releasing Hormone (GnRH)-receptor antagonists. Moreover, the reaction conditions can affect a direct regioselective C–H iodination of the benzimidazole, leading to a range of novel iodo-analogues. The methodologies are powerful strategies for late-stage 123 I-labelling of complex bioactives. Our investigations have generated two highly… Expand
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