Yamamoto F, Sasaki S, Maeda M
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Int J Rad Appl Instrum A. 1992 May;43(5):633-9. doi: 10.1016/0883-2889(92)90032-a.
A one-pot synthesis of 6-deoxy-6-[18F]fluoro-L-ascorbic acid (18F-DFA) has been developed via nucleophilic displacement of a cyclic sulfate with no-carrier-added [18F]fluoride ion. Isolated radiochemical yields of around 15% were obtained with radiochemical purity of over 99% after overall synthesis time of 90 min. Tissue distribution studies with 18F-DFA in rats showed high uptake of radioactivity in the adrenals, kidneys, liver and small intestine--organs known to have high concentrations of L-ascorbic acid. The slow and low uptake of radioactivity in the brain was observed between 10 and 120 min after i.v. injection. In vivo behavior of 18F-DFA in mice bearing 3-methylcholanthrene-induced fibrosarcoma demonstrated its ability to accumulate in the tumor.
通过无载体添加的[¹⁸F]氟离子对环状硫酸酯进行亲核取代反应，开发了一种一锅法合成6-脱氧-6-[¹⁸F]氟-L-抗坏血酸（¹⁸F-DFA）的方法。在90分钟的总合成时间后，获得了约15%的分离放射化学产率，放射化学纯度超过99%。用¹⁸F-DFA对大鼠进行的组织分布研究表明，肾上腺、肾脏、肝脏和小肠（已知含有高浓度L-抗坏血酸的器官）对放射性有高摄取。静脉注射后10至120分钟内，观察到大脑对放射性的摄取缓慢且较低。¹⁸F-DFA在携带3-甲基胆蒽诱导的纤维肉瘤的小鼠体内的行为表明其能够在肿瘤中蓄积。
