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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| Hauptverfasser: | , , , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Französisch |
| Veröffentlicht: |
30 October 2000
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| In: |
Journal of labelled compounds and radiopharmaceuticals
Year: 2000, Jahrgang: 43, Heft: 12, Pages: 1211-1218 |
| ISSN: | 1099-1344 |
| DOI: | 10.1002/1099-1344(20001030)43:12<1211::AID-JLCR408>3.0.CO;2-# |
| Online-Zugang: | 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 |
| Verfasserangaben: | C. Wodarski, J. Eisenbarth, K. Weber, M. Henze, U. Haberkorn and M. Eisenhut |
MARC
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| 245 | 1 | 0 | |a Synthesis of 3'-deoxy-3'-(18F)fluoro-thymidine with 2,3'-anhydro-5'-O-(4,4'-dimethoxytrityl)-thymidine |c C. Wodarski, J. Eisenbarth, K. Weber, M. Henze, U. Haberkorn and M. Eisenhut |
| 246 | 3 | 3 | |a Synthesis of 3'-deoxy-3'- (18 F)fluoro-thymidine with 2,3'-anhydro-5'-O-(4,4'-dimethoxytrityl)-thymidine |
| 264 | 1 | |c 30 October 2000 | |
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| 520 | |a [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. | ||
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| 650 | 4 | |a PET imaging | |
| 650 | 4 | |a Proliferation Marker | |
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