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半自动化合成N-琥珀酰亚胺-4-18F-氟苯甲酸酯
引用本文:张赟,吴战宏,傅喆,李方,朱立,王世真. 半自动化合成N-琥珀酰亚胺-4-18F-氟苯甲酸酯[J]. 同位素, 2009, 22(1): 0-64
作者姓名:张赟  吴战宏  傅喆  李方  朱立  王世真
作者单位:中国医学科学院,中国协和医科大学,北京协和医院,核医学科,北京,100730
基金项目:北京市自然科学基金,北京协和医院青年基金 
摘    要:通过对现有半自动化学合成模块(CPCU)的改造,以乙基-4-三甲胺苯甲酸酯-三氟磺酸盐为反应前体合成用于标记蛋白质、抗体及多肽等牛物分子的辅助基团N-琥珀酰亚胺-4-18F-氟苯甲酸酯(18F-SFB),产物用高效液市H色谱(HPLC)进行检测。合成过程在80min内完成,校正后得到中间产物18F-FBA,产率为80%±5%(n=8),而终产品18F-SFB总衰变校正后的放化收率为40%±5%(n=20),放化纯度≥99%。利用CPCU半自动化合成18F-SFB,方法简便,产率稳定。该法为将来多肽等生物分子的,SF标记提供了依据。

关 键 词:N-琥珀酰亚胺-4-^18F-氟苯甲酸酯(^18F-SFB)  放射性合成  计算机控制化学合成模块(CPCU)
收稿时间:2008-08-25

Radiosynthesis of N-succunimidy-4-18F-fluorobenzoate Using Siemens Chemistry Process Control Unit
ZHANG Yun,WU Zhan-hong,FU Zhe,LI Fang,ZHU Li,WANG Shi-zhen. Radiosynthesis of N-succunimidy-4-18F-fluorobenzoate Using Siemens Chemistry Process Control Unit[J]. Isotopes, 2009, 22(1): 0-64
Authors:ZHANG Yun  WU Zhan-hong  FU Zhe  LI Fang  ZHU Li  WANG Shi-zhen
Affiliation:(Department of Nuclear Medicine, PUMC Hospital, CAMS and PUMC,Beijing 100730, China)
Abstract:The objective of this research was to synthesize the N-succunimidy-4-18F- Fluorobenzoate (18F-SFB), which is used as the prosthetic groups for the 18F labeling of bimolecular like proteins, mono-antibodies and peptides, using the modified Chemistry Process Control Unit (CPCU). The CPCU was modified, we synthesized 18F-SFB using the ethyl-4-trimethyammonium-benzoate triflate as precursor. And the radiochemical purity of the products was measured by High Performance Liquid Chromatograph (HPLC). The total synthesis time was 80 min after EOB. The decay-corrected radiochemical yield of 18F-FBA was 80±5% (n=8) and that of 18F-SFB was 40±5 % (n=20) . The radiochemical purity was more than 99%. Thus, 18F-SFB can be conveniently synthesized with modified CPCU and the labeling yield was stable, which was easily used for the labeling of bioactive compounds.
Keywords:N-succunimidy-4-18F-Fluorobenzoate(18F-SFB)  Radiosynthesis  Chemistry Process Control Unit (CPCU)
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