Production of 18F-Labeled Radiopharmaceuticals
Production of 18F-Labeled Radiopharmaceuticals
Production of 18F-Labeled Radiopharmaceuticals
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Aromatic Radi<strong>of</strong>luorination (4)<br />
- By [ 18 F]acetyl hyp<strong>of</strong>luorite<br />
Addition–elimination mechanism (in freon)<br />
R R<br />
OAc 18 F<br />
R<br />
MeCOO 18 F +<br />
H<br />
-AcOH<br />
18 F<br />
• Acetyl hyp<strong>of</strong>luorite reacts directly with arenes, but only well with<br />
those that are activated by an electron-donating substituent,<br />
especially alkoxy, acetylamino and hydroxy<br />
• Ortho fluorination generally occurs in strong preference to para<br />
fluorination.<br />
• An addition-elimination mechanism has been proposed to<br />
account for the dominance <strong>of</strong> ortho substitution in freon<br />
Aromatic Radi<strong>of</strong>luorination (4)<br />
- By [ 18 F]acetyl hyp<strong>of</strong>luorite (cont’d)<br />
Single electron transfer mechanism (in acetic acid)<br />
R<br />
R<br />
AcO 18 F<br />
R<br />
+ + AcO - -AcOH R<br />
H 18 F<br />
18 F<br />
+ . + 18 F - + AcO . -H 18 F<br />
R<br />
. + AcO -<br />
R<br />
R<br />
Me<br />
OAc
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