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Synthesis of tritium‐labelled 3′‐azido‐3′‐deoxythymidine
Author(s) -
Sidorov G.V.,
Zverkov Yu.B.,
Myasoedov N.F.,
Jasko M.V.,
Skoblov Yu.S.
Publication year - 2003
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.707
Subject(s) - tritium , chemistry , thymine , residue (chemistry) , chemical synthesis , labelling , specific activity , enzyme , radiochemistry , stereochemistry , organic chemistry , biochemistry , in vitro , dna , physics , nuclear physics
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.