Automated radiosynthesis of two ¹⁸F-labeled tracers containing 3-fluoro-2-hydroxypropyl moiety, [¹⁸F]FMISO and [¹⁸F]PM-PBB3, via [¹⁸F]epifluorohydrin.

ABSTRACT:

Background

[¹⁸F]Fluoromisonidazole ([¹⁸F]FMISO) and 1-[¹⁸F]fluoro-3-((2-((1E,3E)-4-(6-(methylamino)pyridine-3-yl)buta-1,3-dien-1-yl)benzo[d]thiazol-6-yl)oxy)propan-2-ol ([¹⁸F]PM-PBB3 or [¹⁸F]APN-1607) are clinically used radiotracers for imaging hypoxia and tau pathology, respectively. Both radiotracers were produced by direct ¹⁸F-fluorination using the corresponding tosylate precursors 1 or 2 and [¹⁸F]F^-, followed by the removal of protecting groups. In this study, we synthesized [¹⁸F]FMISO and [¹⁸F]PM-PBB3 by ¹⁸F-fluoroalkylation using [¹⁸F]epifluorohydrin ([¹⁸F]5) for clinical applications.

Results

First, [¹⁸F]5 was synt

SUBMITTER: Ohkubo T 

PROVIDER: S-EPMC8272768 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature