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Efficient Access to Deuterated and Tritiated Nucleobase Pharmaceuticals and Oligonucleotides using Hydrogen-Isotope Exchange.

Alberto PalazzoloSophie FeuillastreViktor PfeiferSébastien Garcia-ArgoteDonia BouzouitaSimon TricardCéline CholletElodie MarconDavid-Alexandre BuissonSophie CholetFrançois FenailleGuy LippensBruno ChaudretGrégory Pieters
Published in: Angewandte Chemie (International ed. in English) (2019)
A general approach for the efficient hydrogen-isotope exchange of nucleobase derivatives is described. Catalyzed by ruthenium nanoparticles, using mild reaction conditions, and involving either D2 or T2 as isotopic sources, this reaction possesses a wide substrate scope and a high solvent tolerability. This novel method facilitates the access to essential diagnostic tools in drug discovery and development: tritiated pharmaceuticals with high specific activities and deuterated oligonucleotides suitable for use as internal standards during LC-MS quantification.
Keyphrases
  • drug discovery
  • drinking water
  • gas chromatography
  • randomized controlled trial
  • mass spectrometry
  • high resolution
  • amino acid
  • study protocol
  • placebo controlled
  • simultaneous determination