Production of 18F-Labeled Radiopharmaceuticals
Production of 18F-Labeled Radiopharmaceuticals
Production of 18F-Labeled Radiopharmaceuticals
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[ 18 F]XF Addition to Alkenes<br />
18 F<br />
18 F - /NBS<br />
Br<br />
Anti-Markovnikov<br />
product (AM)<br />
+<br />
Br<br />
18 F<br />
Markovnikov<br />
product (M)<br />
(total 30% radiochemical yield; M: AM = 9)<br />
• The Markovnikov addition product dominates over the anti-<br />
Markovnikov product<br />
• The reaction can be performed CA or NCA<br />
Aromatic Radi<strong>of</strong>luorination (1)<br />
- By [ 18 F]fluorine - mechanism<br />
X<br />
18 F-F<br />
X<br />
δ + 18 F F δ+ +<br />
X<br />
18 F<br />
H<br />
X<br />
18 F<br />
• Some arenes can be directly fluorinated in low but useful yields<br />
• For low temperature (– 78 o C) additions <strong>of</strong> dilute fluorine (0.76%<br />
in N 2<br />
) to a large excess <strong>of</strong> substituted benzene, the<br />
substitution pattern is as expected for electrophilic<br />
substitution and supports the proposal <strong>of</strong> a polar substitution<br />
mechanism (above)
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