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1-[18F]fluoro-2-propanol p-toluenesulfonate: a synthon for the preparation of N-([18F]fluoroisopropyl)amines

✍ Scribed by Tjibbe J. De Groot; Philip H. Elsinga; Gerben M. Visser; Willem Vaalburg

Publisher: Elsevier Science
Year: 1992
Weight: 288 KB
Volume: 43
Category: Article
ISSN: 0883-2889
DOI: 10.1016/0883-2889(92)90005-y

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✦ Synopsis

The new radiochemical synthon 1-[~SF]fluoro-2-propanol p-toluenesulfonate 2'a is prepared with a radiochemical yield of 45% [corrected for decay to beginning of synthesis (BOS), synthesis time 40 min]. This compound is used to prepare the [~SF]fluoroisopropyl-alkylated derivatives of benzylamine and norephedrine with a yield of 7 and 2% respectively (BOS, synthesis time 90 min). This alkylation reaction with 2'a gives a good perspective for the preparation of [lSF]fluoro-labelled analogues of flvadrenergic receptor binding ligands for PET. Table I. Attempted conversion of l to 2a

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