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Synthesis and characterization of 2,6-difluoro-4-carboxyphenylboronic acid and a biotin derivative thereof as captors of anionic aqueous [F-18]-fluoride for the preparation of [F-18/F-19]-labeled aryltrifluoroborates with high kinetic stability

TitleSynthesis and characterization of 2,6-difluoro-4-carboxyphenylboronic acid and a biotin derivative thereof as captors of anionic aqueous [F-18]-fluoride for the preparation of [F-18/F-19]-labeled aryltrifluoroborates with high kinetic stability
Publication TypeJournal Article
Year of Publication2008
AuthorsHarwig, CW, Ting, R, Adam, MJ, Ruth, TJ, Perrin, DM
JournalTetrahedron Letters
Volume49
Pagination3152-3156
Date PublishedMay
Type of ArticleArticle
ISBN Number0040-4039
Abstract

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 [F-18]-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. (C) 2008 Published by Elsevier Ltd.

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