Perlmutter M, Satyamurthy N, Luxen A, Phelps M E, Barrio J R
Department of Radiological Sciences, UCLA School of Medicine 90024.
Int J Rad Appl Instrum A. 1990;41(9):801-7. doi: 10.1016/0883-2889(90)90056-m.
4-[18F]Fluoro-L-m-tyrosine (6), a new analog of L-dopa for probing the presynaptic dopaminergic system by positron emission tomography has been synthesized in good radiochemical yields via the regioselective fluorodemercuration of the 4-mercurio derivatives 4a and 4b with 18F-labeled acetylhypofluorite. The chemical, radiochemical and enantiomeric purities were determined to be greater than 99%. The key step in the synthesis of the precursors 4 was the mercuration of the protected L-m-tyrosine 3. The position of mercuration on the aromatic ring was gleaned from the 13C-NMR spectral data. The non-radiolabeled counterpart of 6 was also synthesized. Structural analyses of all these compounds were carried out by 1H-, 13C-, 19F-NMR and mass spectroscopy.
4-[18F]氟-L-间酪氨酸（6）是一种用于通过正电子发射断层扫描探测突触前多巴胺能系统的新型L-多巴类似物，它通过用18F标记的乙酰次氟酸对4-汞衍生物4a和4b进行区域选择性氟脱汞反应，以良好的放射化学产率合成。化学纯度、放射化学纯度和对映体纯度均测定为大于99%。前体4合成中的关键步骤是保护的L-间酪氨酸3的汞化反应。芳香环上汞化的位置从13C-NMR光谱数据中获得。还合成了6的非放射性标记对应物。所有这些化合物的结构分析通过1H-、13C-、19F-NMR和质谱进行。
