Details

Autor(en) / Beteiligte

• Palazzolo, Alberto
• Feuillastre, Sophie
• Pfeifer, Viktor
• Garcia‐Argote, Sébastien
• Bouzouita, Donia
• Tricard, Simon
• Chollet, Céline
• Marcon, Elodie
• Buisson, David‐Alexandre
• Cholet, Sophie
• Fenaille, François
• Lippens, Guy
• Chaudret, Bruno
• Pieters, Grégory

Titel

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

Ist Teil von

• Angewandte Chemie (International ed.), 2019-04, Vol.58 (15), p.4891-4895

Auflage

International ed. in English

Ort / Verlag

Germany: Wiley Subscription Services, Inc

Erscheinungsjahr

2019

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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. Making the swap: A general approach for the late‐stage 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.