Synthesis of 18F labelled nucleoside analogues

Article abstract of DOI:10.1002/(SICI)1099-1344(199612)38:12<1061::AID-JLCR929>3.0.CO;2-J

Several nucleoside analogues like 1-(β-D-glucopyranosyl)-5-fluorouracil 10, 1-(β-D-galactopyranosyl)-5-fluorouracil 11 and 1-(2-deoxy-β-D-glucopyranosyl)- 5-fluorouracil 12 have been synthesized. From the corresponding 1-(2',3',4',6'-tetra-O-acetyl-β-D-glycopyranosyl)-uracil 4, 5 and 6, the ¹⁸F labelled compounds 16, 17 and 18 have been prepared via the intermediates 13, 14 and 15 in acetic acid using [¹⁸F]F₂ and acidic deacetylating procedures. The ¹⁸F labelled derivatives could be obtained, following preparative chromatography, in high purity and in yields of about 3.10⁸ Bq - 5.7·10⁸ Bq (18% - 34% related to the trapped radioactivity, not corrected for decay) for their in-vine evaluation and for in-vivo studies with PET.