Production of 18F-Labeled Radiopharmaceuticals
Production of 18F-Labeled Radiopharmaceuticals
Production of 18F-Labeled Radiopharmaceuticals
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'Electrophilic' Addition<br />
- Some radiopharmaceuticals prepared by<br />
addition <strong>of</strong> [ 18 F]fluorine to alkenes<br />
O<br />
HN<br />
18<br />
F<br />
O<br />
18<br />
F<br />
Me<br />
N<br />
N Me<br />
Ph<br />
O<br />
HN<br />
O<br />
N<br />
H<br />
18<br />
F<br />
HOCH 2<br />
O<br />
O<br />
OH<br />
N<br />
Antipyrine 5-Fluoro-uracil 5-Fluorothymidine<br />
'Electrophilic' Addition<br />
- Preparation <strong>of</strong> FDG by [ 18 F]fluorine addition<br />
CH 2 OAc CH 2 OAc CH 2 OAc<br />
O 18 F-F<br />
O<br />
O<br />
OAc<br />
OAc + OAc<br />
AcO<br />
AcO<br />
18 F AcO F<br />
F<br />
18 F<br />
CH 2 OH<br />
H + O<br />
OH<br />
HO<br />
18 F<br />
H,OH<br />
CH 2 OH<br />
O<br />
+ OH<br />
HO<br />
F<br />
H,OH<br />
• Syn addition to the least hindered face <strong>of</strong> the substrate occurs<br />
preferentially<br />
• Hence, FDG is produced in ninefold greater yield than its 2-epimer,<br />
[ 18 F]2-fluoro-2-deoxy-D-mannose<br />
• Radiochemical yield is 10%
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