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Kit formulation for the preparation of radiolabeled iododeoxyuridine by demetallation
C F Foulon1, S J Adelstein, A I Kassis
1Harvard Medical School, Boston, Massachusetts, USA.
Unlabelled:
The fastest and most reliable preparation of radiolabeled 5-iodo-2'- deoxyuridine (*IUdR) is accomplished by iododemetallation.
Methods:
We describe a kit formulation for the preparation of *IUdR by demercuration whereby [123I/125I/131I]IUdR is synthesized virtually instantaneously following the incubation of an aqueous solution of the chloromercuric precursor with Na123I/125I/131I in the presence of lodogen. We also report the conditions for the radiosynthesis of IUdR by destannylation of the tributylstannyl precursor using hydrogen peroxide as the oxidant.
Results:
In each case, the total procedure is completed in 5 min. HPLC indicates the total transformation of iodide into IUdR with no detectable UV-absorbing by-products. The metal content of the sample is low. The product, therefore, does not require purification.
Conclusion:
*IUdR can be prepared instantly, by either demercuration of ClHgUdR or destannylation of Bu3SnUdR. The use of a mercuric precursor favors a kit formulation since the metallic derivative is stable when kept in aqueous solution, aliquoted in vials coated with the oxidant, for up to 3 mo.