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Synthesis of 18 F labelled nucleoside analogues
Author(s) -
Haeckel Roland,
Weber Klaus,
Germann Christine,
Haberkorn Uwe,
Zeisler Stefan,
Eisenbarth Joseph,
Wiessler Manfred,
Oberdorfer Franz
Publication year - 1996
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199612)38:12<1061::aid-jlcr929>3.0.co;2-j
Subject(s) - chemistry , nucleoside , in vivo , acetic acid , nucleoside analogue , stereochemistry , in vitro , specific activity , organic chemistry , biochemistry , enzyme , microbiology and biotechnology , biology
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)‐uracils 4, 5 and 6 , the 18 F labelled compounds 16, 17 and 18 have been prepared via the intermediates 13, 14 and 15 in acetic acid using [ 18 F]F 2 and acidic deacetylating procedures. The 18 F labelled derivatives could be obtained, following preparative chromatography, in high purity and in yields of about 3·10 8 Bq – 5.7.·10 8 Bq (18% – 34% related to the trapped radioactivity, not corrected for decay) for their in‐vitro evaluation and for in‐vivo studies with PET.