An Organotrifluoroborate for Broadly Applicable One‐Step 18F‐Labeling1. (4th September 2014)

• Record Type: Journal Article
• Authors: Liu, Zhibo; Pourghiasian, Maral; Radtke, Mark Alex; Lau, Joseph; Pan, Jinhe; Dias, Gemma M.; Yapp, Donald; Lin, Kuo‐Shyan; Bénard, Francois; Perrin, David M.
• Is Part Of: Angewandte Chemie. Volume 126:Number 44(2014)
• Page Start: 12070
• Page End: 12074
• Publication Date: 2014-09-04
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1002/ange.201406258
• Languages: English
• ISSNs: 0044-8249

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>A new zwitterionic organotrifluoroborate is appended to three radiosynthons that afford undergo facile bioconjugation to several clinically relevant peptides and one enzyme inhibitor. Molecularly complex bioconjugates are ¹⁸F‐labeled in a single aqueous step in rapid time (&lt;15 min) without HPLC purification to afford tracers in good yields (&gt;200 mCi, 20–40 %) at high specific activity (≥3 Ci/μmol) and at &gt;98 % purity. PET imaging shows in vivo stability and tumor uptake.</p> </abstract>