Multifunctional Deuterated and Tritiated “Click” Molecular Probes via Pd-mediated Reductive De-iodination of 5-Iodo-1,2,3-Triazoles

Andrea Testa, Monica Piras, Mike J Hickey, Ian N. Fleming, Nicholas Bushby, Eva Lenz, Charles S. Elmore, Matteo Zanda

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Abstract

Tritiated compounds are invaluable tools for in vitro and in vivo studies on bioactive molecules. Here we describe a ‘click-chemistry’-based strategy for deuteration and tritiation of multifunctional compounds and multimodal molecular imaging probes. The method relies on a palladium-mediated reductive deiodination of 5-iodo-1,2,3-triazoles in the presence of NaBD4, deuterium or tritium gas.
Original languageEnglish
Pages (from-to)1019-1025
Number of pages7
JournalSynlett
Volume25
Issue number07
DOIs
Publication statusPublished - Apr 2014

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Keywords

  • tritium
  • ‘click’ chemistry
  • 1,2,3-triazole
  • deuterium
  • bioconjugation

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