✦ LIBER ✦
Synthesis and characterization of 2,6-difluoro-4-carboxyphenylboronic acid and a biotin derivative thereof as captors of anionic aqueous [18F]-fluoride for the preparation of [18F/19F]-labeled aryltrifluoroborates with high kinetic stability
✍ Scribed by Curtis W. Harwig; Richard Ting; Michael J. Adam; Thomas J. Ruth; David M. Perrin
- Publisher
- Elsevier Science
- Year
- 2008
- Tongue
- French
- Weight
- 154 KB
- Volume
- 49
- Category
- Article
- ISSN
- 0040-4039
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✦ Synopsis
Arylboronic esters are readily converted to aryltrifluoroborates in the presence of aqueous fluoride. As such these represent attractive synthetic precursors that afford one-step labeling with [ 18 F]-fluoride for the generation of PET reagents. Herein we present the synthesis of a heretofore undisclosed arylboronic ester that is converted to its corresponding trifluoroborate. Essential for contemplating its use in PET imaging is the demonstration of kinetic resistance to solvolytic defluoridation.