作者:Michael A. Carroll、James Nairne、John L. Woodcraft
DOI:10.1002/jlcr.1190
日期:2007.4
Fluorine-18 labelled fluoropyridines have found increasing application in the medical imaging technique of Positron Emission Tomography. The fluorine-18 has largely been restricted to the 2- and 6-position where its introduction may be readily achieved, from a range of appropriate precursors, by nucleophilic aromatic substitution using [18F]fluoride. However, fluorine at this position may be labile in vivo limiting the potential of the radiotracer. To date the more stable 3-fluoro and 5-fluoropyridines have not been exploited due to unsuitable methods of preparation. Pyridyliodonium salts provide a convenient way to overcome this restriction and allow the introduction of fluorine-18, as fluoride, into the 3- or 5-position. Copyright © 2007 John Wiley & Sons, Ltd.
氟-18 标记的氟吡啶在正电子发射断层扫描医学成像技术中的应用越来越广泛。氟-18 在很大程度上被限制在 2-位和 6-位,在这两个位置上,通过使用[18F]氟化物进行亲核芳香取代,可以很容易地从一系列适当的前体中引入氟-18。然而,这个位置的氟在体内可能是易变的,从而限制了放射性示踪剂的潜力。迄今为止,由于制备方法不合适,更稳定的 3-氟和 5-氟吡啶还没有被利用。吡啶碘鎓盐提供了一种方便的方法来克服这一限制,并允许将氟-18 以氟化物的形式引入 3 位或 5 位。版权所有 © 2007 John Wiley & Sons, Ltd. 保留所有权利。