Rapid and efficient synthesis of [18F]fluoronicotinamides, [18F]fluoroisonicotinamides and [18F]fluorobenzamides as potential pet radiopharmaceuticals for melanoma imaging
Rapid and efficient synthesis of [18F]fluoronicotinamides, [18F]fluoroisonicotinamides and [18F]fluorobenzamides as potential pet radiopharmaceuticals for melanoma imaging
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DOI：
10.1002/jlcr.1869
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发表时间：
2011-05-01
影响因子：
1.8
通讯作者：
Amartey, J.
中科院分区：
文献类型：
--
作者：
Al Jammaz, I.;Al-Otaibi, B.;Amartey, J.
为了简化亲核放射性氟化反应以使其适合自动化，使用一步合成方法合成了一系列[F-18]氟烟酰胺、[F-18]氟异烟酰胺和[F-18]氟苯甲酰胺，该方法涉及三甲基铵-烟酰胺、三甲基铵-异烟酰胺和三甲基铵-苯甲酰胺前体的置换反应。基于起始的[F-18]-氟化物，在20分钟合成时间内并且无需高效液相色谱纯化，放射化学产率和纯度分别大于90%和97%。这种合成方法作为一种快速、简单的方法，有望成为自动放射性氟化 [F-18] 氟烟酰胺、[F-18] 氟异烟酰胺和 [F-18] 氟苯甲酰胺的方法，具有高放射化学收率和非常短的制备时间。
In an attempt to simplify nucleophilic radiofluorination reactions to be amenable for automation, a series of [F-18]fluoronicotinamides, [F-18]fluoroisonicotinamides and [F-18]fluorobenzamides were synthesized using one-step synthetic approach involving displacement reactions on trimethylammonium-nicotinamide, trimethylammonium-isonicotinamide and trimethylammonium-benzamide precursors. Based on starting [F-18]-fluoride, radiochemical yields and purities were found to be greater than 90 and 97%, respectively, within 20 min synthesis time and, without high-performance liquid chromatography purification. This synthetic approach holds great promise as a rapid and simple method for the automated radiofluorination of [F-18]fluoronicotinamides, [F-18]fluoroisonicotinamides and [F-18]fluorobenzamides with high radiochemical yield and very short preparation time.