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在柱水解法自动化合成2-^18F-2-脱氧-D-葡萄糖
引用本文:罗磊,;唐刚华,;唐小兰. 在柱水解法自动化合成2-^18F-2-脱氧-D-葡萄糖[J]. 湖南医科大学学报, 2009, 0(11): 1151-1156
作者姓名:罗磊,  唐刚华,  唐小兰
作者单位:[1]湖南省肿瘤医院PET—CT中心,长沙410013; [2]中山大学附属第一医院核医学科PET中心,广州510080; [3]华南农业大学理学院应用化学系,广州510642
摘    要:目的:研究在柱水解法自动化合成2-18F-2-脱氧-D-葡萄糖(2-[18F]-fluoro-2-deoxy-D-glu-cose,18F-FDG)。方法:采用在柱水解法和TRACERlabFXF-N自动化合成仪,以三氟甘露糖为前体,经亲核氟化、氢氧化钠在柱水解两步反应及SEP-PAK小柱分离纯化制备18F-FDG注射液。结果:18F-FDG总合成时间小于20min,未校正放化产率大于60%,放化纯度大于99%。结论:在柱水解法合成18F-FDG注射液,操作简便,是很实用的18F-FDG生产方法。合成的18F-FDG注射液可用于临床PET显像研究。

关 键 词:2-18F-2-脱氧-D-葡萄糖  在柱水解法  自动化合成

Automated synthesis of 2-[^18F]-fluoro-2-deoxy-D-glucose by on-column hydrolysis
Affiliation:LUO Lei, TANG Ganghua , TANG Xiaolan ( 1. PET-CT Centre, Hunan Tumour Hospital, Changsha 410013; 2. PET-CT Centre, First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080 ; 3. Department of Applied Chemistry, College of Sciences, South China Agricultural University, Guangzhou 510642, China )
Abstract:Objective To study automated synthesis of 2- [^18 F ] -fluoro-2 -deoxy-D-glucose (^18 F-FDG) via on-column hydrolysis. Methods Automated synthesis of ^18 F-FDG was performed by the on-column hydrolysis procedure in TRACERIab FXF-N synthesizer, ^18F-FDG injection was obtained via nucleophilic fluorination of 1, 3, 4, 6-tetra-O-acetyl-2-O-trifluoromethanesulfony-β-D-mannopyranose as the precursor molecule with ^18F-fluoride, hydrolysis of the ^18F-labeled intermediate on SEP-PAK C18 cartridges with 2 mol/L NaOH solution, and purification and neutralization with SEP-PAK cartridges. Results The uncorrected radiochemical yield of ^18F-FDG was more than 60% within the total synthesis time shorter than 20 min. The radiochemical purity of ^18F-FDG was above 99%. Conclusion On-column hydrolysis is simple and practical for the automated synthesis of ^18F-FDG. ^18F-FDG injection produced by this procedure can be used in clinical PET imaging.
Keywords:2- -fluoro-2-deoxy-D-glucose  on-column hydrolysis  fully automated synthesis
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