Abstract : 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.
https://hal-cea.archives-ouvertes.fr/cea-02075752 Contributor : Marianne LericheConnect in order to contact the contributor Submitted on : Thursday, March 21, 2019 - 3:44:49 PM Last modification on : Monday, July 4, 2022 - 9:19:35 AM Long-term archiving on: : Saturday, June 22, 2019 - 3:20:02 PM
Alberto Palazzolo, Sophie Feuillastre, Viktor Pfeifer, Sébastien Garcia-Argote, Donia Bouzouita, et al.. Efficient Access to Deuterated and Tritiated Nucleobase Pharmaceuticals and Oligonucleotides using Hydrogen-Isotope Exchange. Angewandte Chemie International Edition, Wiley-VCH Verlag, 2019, 58 (15), pp.4891-4895. ⟨10.1002/anie.201813946⟩. ⟨cea-02075752⟩