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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.

SUBMITTER: Palazzolo A

PROVIDER: S-EPMC6593778 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

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

Palazzolo Alberto A Feuillastre Sophie S Pfeifer Viktor V Garcia-Argote Sébastien S Bouzouita Donia D Tricard Simon S Chollet Céline C Marcon Elodie E Buisson David-Alexandre DA Cholet Sophie S Fenaille François F Lippens Guy G Chaudret Bruno B Pieters Grégory G

Angewandte Chemie (International ed. in English) 20190306 15

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 deuterat ...[more]

PMID: 30768844

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