Bishop A, Satyamurthy N, Bida G, Barrio J R
Department of Molecular and Medical Pharmacology, UCLA School of Medicine, USA.
Nucl Med Biol. 1996 Jul;23(5):559-65. doi: 10.1016/0969-8051(95)02073-x.
A comprehensive evaluation of the reactivity of 18F electrophilic fluorinating agents derived from the 18O(p,n)18F reaction conducted in target bodies made of aluminum, silver, copper, nickel, and gold-plated copper is reported. Two representative electrophilic reactions, namely addition across a double bond and substitution on an aromatic ring (fluorodemercuration and fluorodestannylation), were tested with the 18F activity generated in the [18O]O2 target systems. Identical reactions were also conducted with analogous nonradioactive fluorinating agents as control experiments. The products of all these reactions were analyzed by NMR spectroscopy. Results of these experiments clearly showed that 18F activities recovered from aluminum, silver, and copper target bodies were better suited for radiochemical syntheses, irrespective of the irradiation protocols employed. The 18F activity from a gold-plated target was suitable only for addition reactions. Further, the fluorodemercuration reaction essentially failed with the single-step irradiation technique conducted in nickel and gold-plated targets. In contrast, the fluorodestannylation reaction was quite successful with the 18F reagents recovered from all the target bodies and irradiation protocols.
报道了对在由铝、银、铜、镍和镀铜制成的靶体中进行的(^{18}O(p,n)^{18}F)反应衍生的18种亲电氟化剂的反应活性进行的综合评估。用([^{18}O]O_2)靶系统中产生的(^{18}F)活性测试了两种代表性的亲电反应，即双键加成和芳环上的取代反应（氟脱汞反应和氟脱锡反应）。还使用类似的非放射性氟化剂进行了相同的反应作为对照实验。所有这些反应的产物均通过核磁共振光谱进行分析。这些实验结果清楚地表明，从铝、银和铜靶体中回收的(^{18}F)活性更适合放射化学合成，与所采用的辐照方案无关。镀铜靶体产生的(^{18}F)活性仅适用于加成反应。此外，在镍和镀铜靶体中采用单步辐照技术时，氟脱汞反应基本失败。相比之下，从所有靶体和辐照方案中回收的(^{18}F)试剂进行氟脱锡反应非常成功。
