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Synthesis of 3'-deoxy-3'-(18F)fluoro-thymidine with 2,3'-anhydro-5'-O-(4,4'-dimethoxytrityl)-thymidine

[11C]Thymidine has been used as a proliferation marker in positron-emission-tomography (PET) studies of tumors. This compound showed metabolite related problems and the radiosynthesis proved to be difficult. Recently, the more stable 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT) has been suggested as...

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Bibliographic Details
Main Authors: Wodarski, Christine (Author) , Eisenbarth, Joseph (Author) , Weber, Klaus-Josef (Author) , Henze, Marcus (Author) , Haberkorn, Uwe (Author) , Eisenhut, Michael (Author)
Format: Article (Journal)
Language:French
Published: 30 October 2000
In: Journal of labelled compounds and radiopharmaceuticals
Year: 2000, Volume: 43, Issue: 12, Pages: 1211-1218
ISSN:1099-1344
DOI:10.1002/1099-1344(20001030)43:12<1211::AID-JLCR408>3.0.CO;2-#
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1002/1099-1344(20001030)43:12<1211::AID-JLCR408>3.0.CO;2-%23
Verlag, lizenzpflichtig, Volltext: https://onlinelibrary.wiley.com/doi/abs/10.1002/1099-1344%2820001030%2943%3A12%3C1211%3A%3AAID-JLCR408%3E3.0.CO%3B2-%23
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Author Notes:C. Wodarski, J. Eisenbarth, K. Weber, M. Henze, U. Haberkorn and M. Eisenhut
Description
Summary:[11C]Thymidine has been used as a proliferation marker in positron-emission-tomography (PET) studies of tumors. This compound showed metabolite related problems and the radiosynthesis proved to be difficult. Recently, the more stable 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT) has been suggested as an alternative. One advantage of [18F]FLT is based on thymidine kinase-1 catalyzed phosphorylation of FLT and the intracellular accumulation of this metabolite without participation in DNA synthesis. The radiosynthesis of [18F]FLT originally designed by Grierson et al. was found to be demanding especially regarding the workup of the [18F]fluoride/1-(2-deoxy-3-O-nosyl-5-O-DMT-β-D-threo-pento-furanosyl)-3-DMBn-thymine reaction mixture. Instead, we used 2,3′-anhydro-5′-O-(4,4′-dimethoxytrityl)thymidine as a precursor for the synthesis of [18F]FLT. In DMSO at 175°C and in presence of Kryptofix® 2.2.2. we obtained 5.6± 1,4% [18F]FLT (EOS). Copyright © 2000 John Wiley & Sons, Ltd.
Item Description:Im Titel steht der Ausdruck (18F) in eckiger Klammer, die Zahl 18 ist dabei hochgestellt
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Physical Description:Online Resource
ISSN:1099-1344
DOI:10.1002/1099-1344(20001030)43:12<1211::AID-JLCR408>3.0.CO;2-#

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