DeJesus O T, Sunderland J J, Nickles J R, Mukherjee J, Appelman E H
Department of Medical Physics, University of Wisconsin-Madison 53706.
Int J Rad Appl Instrum A. 1990;41(5):433-7. doi: 10.1016/0883-2889(90)90001-w.
The direct electrophilic radiofluorination of m-tyrosine using [18F]acetylhypofluorite was investigated. Results showed that this reaction was both rapid and efficient with recovered decay corrected yield of 71% radiofluorinated m-tyrosines based on starting [18F]acetylhypofluorite. Specific activity of the product obtained in this study was 100-200 mCi/mmol although 1-5 Ci/mmol are easily achievable with our improved production of [18F]AcOF. Three positional isomers were found and identified by 19F-NMR to be 2-, 4-, 6-fluoro-m-tyrosine with a distribution of 36:11:52, respectively. This measured distribution allowed the assignment of the radio-HPLC peaks. Biological studies are currently underway in our laboratory using these fluoro-m-tyrosines to determine which isomer would be most suited for the evaluation of the dopamine system by positron tomography.
研究了使用[¹⁸F]乙酰次氟酸对间酪氨酸进行直接亲电放射性氟化反应。结果表明，该反应迅速且高效，基于起始的[¹⁸F]乙酰次氟酸，经衰变校正后回收的放射性氟化间酪氨酸产率为71%。本研究中获得的产物比活度为100 - 200 mCi/mmol，不过通过我们改进的[¹⁸F]AcOF制备方法，1 - 5 Ci/mmol很容易实现。通过¹⁹F - NMR发现并鉴定出三种位置异构体，分别为2 - 、4 - 、6 - 氟间酪氨酸，其分布比例为36:11:52。这种测量得到的分布情况有助于确定放射性高效液相色谱峰。我们实验室目前正在进行生物学研究，使用这些氟代间酪氨酸来确定哪种异构体最适合通过正电子断层扫描评估多巴胺系统。
