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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]. 中南大学学报(医学版), 2009, 34(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-glucose, 18F-FDG)。方法:采用在柱水解法和TRACERlab FXF-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20 min,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  
收稿时间:2008-10-13

Automated synthesis of 2-[~(18)F]-fluoro-2-deoxy-D-glucose by on-column hydrolysis
LUO Lei,TANG Ganghua,TANG Xiaolan. Automated synthesis of 2-[~(18)F]-fluoro-2-deoxy-D-glucose by on-column hydrolysis[J]. Journal of Central South University. Medical sciences, 2009, 34(11): 1151-1156
Authors:LUO Lei  TANG Ganghua  TANG Xiaolan
Affiliation: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:ObjectiveTo study automated synthesis of 2-[18F]-fluoro-2-deoxy-D-glucose (18F-FDG) via on-column hydrolysis. MethodsAutomated synthesis of 18F-FDG was performed by the on-column hydrolysis procedure in TRACERlab 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.ResultsThe 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%. ConclusionOn-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-[18F]-fluoro-2-deoxy-D-glucose;on-column hydrolysis;fully automated synthesis
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