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Efficient Access to Deuterated and Tritiated Nucleobase Pharmaceuticals and Oligonucleotides using Hydrogen‐Isotope Exchange |
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| Authors: | Alberto Palazzolo Sophie Feuillastre Viktor Pfeifer Sbastien Garcia‐Argote Donia Bouzouita Simon Tricard Cline Chollet Elodie Marcon David‐Alexandre Buisson Sophie Cholet Franois Fenaille Guy Lippens Bruno Chaudret Grgory Pieters |
| Institution: | Alberto Palazzolo,Sophie Feuillastre,Viktor Pfeifer,Sébastien Garcia‐Argote,Donia Bouzouita,Simon Tricard,Céline Chollet,Elodie Marcon,David‐Alexandre Buisson,Sophie Cholet,François Fenaille,Guy Lippens,Bruno Chaudret,Grégory Pieters |
| 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. |
| Keywords: | C-H-Aktivierung Isotope Isotopenmarkierung Nanopartikel Nukleotide |