Synthesis of tritium-labeled nucleoside 5′-triphosphates and nucleoside 5′-diphosphates

Abstract

Tritium-labeled nucleoside 5′-triphosphates (NTPs) nucleoside 5′-diphosphates (NDPs) containing the tritium label in positions 8 (in the purine nucleus) and 5 (in the pyrimidine nucleus) have been obtained by the dehalogenation of the corresponding bromine derivatives with gaseous tritium. The dehalogenation of the Br-NTPs and Br-NDPs was carried out at atmospheric pressure in an aqueous alkaline medium using palladium catalysts (5% Pd/BaSO4 or α-Pd). The possibility of introducing a tritium label into nucleotides of the adenine series by the heterogenecus isotope exchange reaction with gaseous tritium in the presence of 5% Pd/BaSO4 has been investigated. For the compounds synthesized, the compositions of the eluents used for the chromatographic isolation of the desired products are given. The molar activities of the compounds synthesized were between 370 and 740 TBq/mole (10–20 kCi/mole).