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

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.
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Submitted on : Thursday, March 21, 2019 - 3:44:49 PM
Last modification on : Monday, July 15, 2019 - 2:20:05 PM
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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, ⟨10.1002/anie.201813946⟩. ⟨cea-02075752⟩

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