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Synthesis and preliminary evaluation of [ 18 F]2‐deoxy‐2,2‐difluoro‐glucose as a potential PET imaging agent
Author(s) -
Adam Michael J.
Publication year - 1999
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(199908)42:8<809::aid-jlcr241>3.0.co;2-8
Subject(s) - chemistry , biodistribution , in vivo , specific activity , yield (engineering) , positron emission tomography , pet imaging , imaging agent , radiochemistry , glucal , nuclear medicine , pharmacology , in vitro , biochemistry , catalysis , medicine , microbiology and biotechnology , biology , materials science , metallurgy , enzyme
This paper describes the synthesis and preliminary in‐vivo study of a new FDG analog, 2‐deoxy‐2,2‐[ 18 F]difluoro‐glucose (DFDG) for use as a potential imaging agent for PET. DFDG was prepared by the reaction of 18 F‐acetyl hypofluorite on 3,4,6‐tri‐ O ‐acetyl‐2‐fluoro‐ D ‐glucal followed by acid deprotection to give the final product in 27% decay corrected radiochemical yield. Biodistribution in mice showed rapid uptake in the heart (10% dose/gram) which remained relatively constant out to two hours. The brain uptake at 2 hours was 1.6% dose per gram. There was rapid clearance of activity from the blood after injection. Brain images in a Rhesus monkey showed a similar distribution when compared to FDG but with significantly more uptake in surrounding muscle. Copyright © 1999 John Wiley & Sons, Ltd.