Production of 18F-Labeled Radiopharmaceuticals
Production of 18F-Labeled Radiopharmaceuticals
Production of 18F-Labeled Radiopharmaceuticals
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[ 18 F]Fluorodemetallation<br />
- General features<br />
• Reactivity is aryl-Hg ~ aryl-Sn > aryl-Ge ~ aryl-Si<br />
i.e. in inverse order <strong>of</strong> aryl C–M bond strength.<br />
• Fluorodemercuration with acetyl hyp<strong>of</strong>luorite is regiospecific<br />
• Aryl-tri-n-butyltins treated with [ 18 F]fluorine or [ 18 F]acetyl<br />
hyp<strong>of</strong>luorite give ipso-substituted [ 18 F]fluoroarenes in<br />
similarly high radiochemical yield (measured from<br />
[ 18 F]fluorine).<br />
• Electron-withdrawing substituents (e.g. 4-CF 3<br />
, 4-CN) reduce the<br />
yield <strong>of</strong> ring radi<strong>of</strong>luorination in aryltrimethyl-tin, -<br />
germanium and -silicon compounds<br />
[ 18 F]Fluorodemetallation<br />
- Synthesis <strong>of</strong> FDOPA<br />
OMe<br />
OMe<br />
OH<br />
MeO<br />
MeO<br />
HO<br />
HgOOCF 3<br />
MeCOO 18 F<br />
18 F<br />
HI<br />
18 F<br />
H<br />
H<br />
H<br />
AcHN<br />
CO 2 Me<br />
AcHN<br />
CO 2 Me<br />
H 2 N<br />
CO 2 H<br />
• FDOPA can be isolated in 12% radiochemical yield (decay<br />
corrected)<br />
• Similar radiosytheses have been devised with alkyl-tin and<br />
alkyl-silicon leaving groups
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