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Synthesis of tritium-labelled 3′-azido-3′-deoxythymidine

✍ Scribed by G.V. Sidorov; Yu.B. Zverkov; N.F. Myasoedov; M.V. Jasko; Yu.S. Skoblov

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
97 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

New approaches to the synthesis of 3′‐azido‐3′‐deoxythymidine labelled with tritium in the heterocyclic base have been developed. With this aim, enzymatic transribosylation with [^3^H]thymine using the enzyme preparation from rat liver and a three‐step chemical synthesis with use of the tritium labelled precursor were studies. The enzyme preparation did not catalyse the transfer of the 3′‐azido‐3′‐deoxyribosyl fragment to the [^3^H]thymine residue. 5′‐O‐Benzoyl‐2,3′‐anhydrothymidine was taken as a precursor for the tritium labelling by the chemical methods. The resulting [^3^H]3′‐azido‐3′‐deoxythymidine was obtained with a specific radioactivity of 18.3 Ci/mmol, the tritium is located in the C‐6 position of the thymine residue. Copyright © 2003 John Wiley & Sons, Ltd.

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