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Direct incorporation of [11C]carbon dioxide for labeling bioactive molecules. An application to [11C] labeled tamoxifen

✍ Scribed by Siya Ram; Leonard D. Spicer


Publisher
John Wiley and Sons
Year
1989
Tongue
French
Weight
256 KB
Volume
27
Category
Article
ISSN
0022-2135

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✦ Synopsis


A one-pot synthesis of [ ' l C ] labeled tamoxifen has been d veloped via reductive carboxylation. In this approach, [ 'C]C02 is reacted with the N-trimethylsilyl derivative of desmethyltamoxifen, followed by in situ sodium bis (2-metho ethoxy)aluminum hydride reduction, to afford impure ["C] labeled tamoxifen, which, on purification 011' a basic alumina-silica gel column, provided pure

[ C] tamoxifen in excellent radiochemical yield ( 6 5 % to 84%) nd radiochemical purity (>99%). The specific activity of [lfCJtamoxifen was 250-400 Ci/mmol at the end of bombardment.