Comparison of pathways to the versatile synthon of no-carrier-added 1-bromo-4-[18F]fluorobenzene
✍ Scribed by Johannes Ermert; Carsten Hocke; Thomas Ludwig; René Gail; Heinz H. Coenen
- Publisher
- John Wiley and Sons
- Year
- 2004
- Tongue
- French
- Weight
- 142 KB
- Volume
- 47
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.830
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✦ Synopsis
Abstract
The availability of no‐carrier‐added (n.c.a.) 1‐bromo‐4‐[^18^F]fluorobenzene with high radiochemical yields is important for ^18^F‐arylation reactions using metallo‐organic 4‐[^18^F]fluorophenyl compounds (e.g. of lithium or magnesium) or Pd‐catalyzed coupling. In this study, different methods for the preparation of 1‐bromo‐4‐[^18^F]fluorobenzene by nucleophilic aromatic substitution reactions using n.c.a. [^18^F]fluoride were examined. Of six pathways compared, symmetrical bis‐(4‐bromphenyl)iodonium bromide proved most useful to achieve the title compound in a direct, one‐step nucleophilic substitution with a radiochemical yield (RCY) of 65% within 10 min. Copyright © 2004 John Wiley & Sons, Ltd.