Efficient access to deuterated and tritiated nucleobase pharmaceuticals and oligonucleotides using hydrogen isotope exchange

A general approach for the nucleobase derivatives hydrogen isotope exchange is described. Catalyzed by ruthenium nanoparticles, using mild reaction conditions and involving D2 or T2 as isotopic sources, this reaction possesses a wide substrate scope and a high solvent tolerability. This novel method facilitates the convenient access to essential diagnostic tools in drug discovery and development: tritiated pharmaceuticals with high specific activities and deuterated oligonucleotides suitable to be used as internal standards for LC‐MS quantification.

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