Hwang D R, Dence C S, Bonasera T A, Welch M J
Edward Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110.
Int J Rad Appl Instrum A. 1989;40(2):117-26. doi: 10.1016/0883-2889(89)90186-x.
Four different approaches towards the synthesis of [18F]FMISO have been studied. The first approach was based on the reaction of epoxide 4 and [18F]fluoride. Both specific activity and radiochemical yield (less than 1%) for [18F]FMISO were low. Two new approaches, starting with compounds 8 and 9, have failed to give [18F]FMISO. The fourth approach, based on the reaction of [18F]epifluorohydrin 10, prepared from Tosylate 13 and [18F]KF/Kryptofix 222, has provided a reliable, no-carrier added synthesis of [18F]FMISO. The product was obtained in a radiochemical yield of 7-12% at end-of-synthesis (based on [18F]fluoride) with a specific activity of greater than 400 Ci/mmol and a synthesis time of 1.5 h. Preliminary PET studies suggest that [18F]FMISO may be a promising tracer for delineation of ischemic but viable myocardium.
研究了四种合成[18F]氟代米索硝唑（[18F]FMISO）的不同方法。第一种方法基于环氧化物4与[18F]氟化物的反应。[18F]FMISO的比活度和放射化学产率（低于1%）都很低。从化合物8和9开始的两种新方法未能得到[18F]FMISO。第四种方法基于由对甲苯磺酸酯13与[18F]氟化钾/穴醚222制备的[18F]环氧氟丙烷10的反应，已提供了一种可靠的、无载体添加的[18F]FMISO合成方法。在合成结束时（基于[18F]氟化物），产物的放射化学产率为7 - 12%，比活度大于400 Ci/mmol，合成时间为1.5小时。初步的正电子发射断层扫描（PET）研究表明，[18F]FMISO可能是一种用于描绘缺血但存活心肌的有前景的示踪剂。
