摘要
目的 研究新的18F多功能模块,以满足临床对多种18F正电子药物的需求.方法 设计的双管18F多功能模块由氟离子捕获、第1反应管、第2反应管、高效液相色谱（HPLC）纯化和固相萃取5个部分组成,反应管透明.采用2个反应管进行不同反应,以制备复杂化合物.结果 采用该模块合成了较复杂的标记多肽或蛋白质的第2标记前体N-琥珀酰亚胺-4-18F-氟苯甲酸酯（SFB）和18F-乙基胆碱,合成了常用药物18F-脱氧葡萄糖（FDG）、3＇-脱氧-3＇-18F-氟代胸苷（FLT）.前三者不校正合成效率分别为（28.2±1.9）%（n=5）、（22.5±3.8）%（n=6）、（58.2±5.4）%（n=32）,18F-FLT校正合成效率为（30.1±6.2）%（n=10）;同时用该模块合成了11C-N-甲基-N-（1-甲基丙基）-1-（2-氯苯基）异喹啉-3-氨甲酰（PK11195）,合成效率为（31.2±2.5）%（n=3）.结论 反应管透明,可判断反应进度.双管多功能反应管可合成复杂的18F药物,以满足临床及科研的需求.
Objective To explore a new 18F multifunctional synthesis module with two vessels to synthesize various kinds of 18F labeled radiopharmaceuticals for clinical utilities. Methods The module with two vessels contained five systems, capture of F ion, the first reaction vessel, the second reaction vessel, high performance liquid chromatography （HPLC） purification, and solid extraction. The two vessels were made of transparent glass and were used to prepare complex products by nucleophilic reaction or hydrolyzation. Results The complex compounds of 18F-ethyl-choline, 18F-N-succinimidyl-4-18 F-fluorobenzoate （SFB）, and common compounds of 18F-fluorodeoxyglucose （FDG）, 18F-3＇-deoxy-3＇-18 F-fluorothymidine （FLT） were synthesized by the new module. The uncorrected synthesis yield （EOS） of 18F-SFB, 18F-ethylcholine, and 18F-FDG were （28.2±1.9）% （n=5）, （22.5±3.8）%（n=6）, and （58.2±5.4）% （n=32）, respectively. The corrected synthesis yield of 18F-FLT was （30.1 ±6.2）% （ n = 10）. In addition,11C-N-methyl-N-（ 1-methylpropyl ）-1-（ 2-corophenyl ）-isoquinoline-3 -carboxamide （ PK11195 ） was also prepared by the module with the yield of （31.2 ± 2.5） % （ n = 3 ）. Conclusions The new module with two vessels has been used for synthesis of many 18F compounds and it may have the potential to be used for other more 18F radiopharmaceuticals.
出处
《中华核医学杂志》
CAS
CSCD
北大核心
2010年第6期410-413,共4页
Chinese Journal of Nuclear Medicine
关键词
放射化学
化学合成
氟放射性同位素
Radiochemistry
Chemical synthesis
Fluorine radioisotopes
