Rapid and efficient synthesis of [18F]fluoronicotinamides, [18F]fluoroisonicotinamides and [18F]fluorobenzamides as potential pet radiopharmaceuticals for melanoma imaging

被引：4
作者：
Al Jammaz, I. [1 ]
Al-Otaibi, B. [1 ]
Okarvi, S. [1 ]
Amartey, J. [1 ]
机构：
[1] King Faisal Specialist Hosp & Res Ctr, Cyclotron & Radiopharmaceut Dept, Riyadh 11211, Saudi Arabia
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2011年 / 54卷 / 06期
关键词：
F-18-fluorination; F-18-fluoronicotinamide; F-18-fluoroisonicotinamide; F-18-fluorobenzamide; melanoma targeting; PET radiopharmaceuticals; MALIGNANT-MELANOMA; IN-VITRO; BIODISTRIBUTION; METASTASES; BENZAMIDES; TRACERS; AGENT;
D O I：
10.1002/jlcr.1869
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
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.
引用
收藏
页码：312 / 317
页数：6
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