Synthesis of 18F labelled nucleoside analogues

✍ Scribed by Roland Haeckel; Klaus Weber; Christine Germann; Uwe Haberkorn; Stefan Zeisler; Joseph Eisenbarth; Manfred Wiessler; Franz Oberdorfer

• Publisher: John Wiley and Sons
• Year: 1996
• Tongue: French
• Weight: 452 KB
• Volume: 38
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/(sici)1099-1344(199612)38:12<1061::aid-jlcr929>3.0.co;2-j

✦ Synopsis

Several nucleoside analogues like l-(~-D-glucopyranosyl)-5-fluorouracil 10, 1-(~-D-galactopyranosy1)-5-fluorouracil 11 and l-(2-deoxy-PD-glucopyranosyl)-5-fluorouracil 12 have been synthesized. From the corresponding 1-(2',3',4',6-tetra-O-acetyl-~-D-glycop~anosyl)-uracils 4, 5

and 6, the I8F labelled compounds 16, 17 and 18 have been prepared via the intermediates 13, 14 and 15 in acetic acid using [18F]b and acidic deacetylating procedures. The l8F labelled derivatives could be obtained, following preparative chromatography, in high purity and in yields of about 3.10s Bq -5.7.108 Bq (18% -34% related to the trapped radioactivity, not corrected for decay) for their in-vitro evaluation and for in-vivo studies with PET.