用[¹⁸F]F₂和[¹⁸F]CH₃COOF进行区域选择性放射性氟脱锡反应：6-[¹⁸F]氟-L-多巴的高产率合成。
Regioselective radiofluorodestannylation with [18F]F2 and [18F]CH3COOF: a high yield synthesis of 6-[18F]Fluoro-L-dopa.
作者信息
Namavari M, Bishop A, Satyamurthy N, Bida G, Barrio J R
机构信息
Department of Radiological Sciences, UCLA School of Medicine.
出版信息
Int J Rad Appl Instrum A. 1992 Aug;43(8):989-96. doi: 10.1016/0883-2889(92)90217-3.
A protected 6-trimethylstannyl dopa derivative 6 has been synthesized for the first time as a precursor for the preparation of 6-[18F]fluoro-L-dopa. The tin derivative 6 readily reacted with electrophilic radiofluorinating agents such as [18F]F2 and [18F]AcOF. The [18F]fluoro intermediate 7 was easily hydrolyzed with HBr and the product 6-[18F]fluoro-L-dopa was isolated after HPLC purification in a maximum radiochemical yield of 25%, ready for human use. The various intermediates, the stannyl precursor 6 and the final product (after 18F decay) were all fully characterized by 1H, 13C, 19F and 119Sn NMR as well as high resolution mass spectroscopy.
首次合成了一种受保护的6 - 三甲基锡基多巴衍生物6，作为制备6 - [¹⁸F]氟 - L - 多巴的前体。锡衍生物6很容易与亲电放射性氟化剂如[¹⁸F]F₂和[¹⁸F]AcOF反应。[¹⁸F]氟中间体7很容易用HBr水解，产物6 - [¹⁸F]氟 - L - 多巴经HPLC纯化后分离得到，最大放射化学产率为25%，可供人体使用。各种中间体、锡基前体6和最终产物（¹⁸F衰变后）均通过¹H、¹³C、¹⁹F和¹¹⁹Sn NMR以及高分辨率质谱进行了全面表征。
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