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简便快速自动化合成报告基因表达PET显像剂18F-FHBG
引用本文:唐刚华,唐小兰,王明芳,李葆元,梁明泉,王全师.简便快速自动化合成报告基因表达PET显像剂18F-FHBG[J].核技术,2009,32(8).
作者姓名:唐刚华  唐小兰  王明芳  李葆元  梁明泉  王全师
作者单位:1. 中山大学附属第一医院核医学科PET-CT中心,广州,510080;南方医科大学南方医院核医学科PET中心,广州,510515
2. 华南农业大学理学院,广州,510642
3. 南方医科大学南方医院核医学科PET中心,广州,510515
基金项目:中山大学"百人计划"引进人才科研启动基金,国家高技术研究发展计划(863计划)专题课题 
摘    要:用一锅法和TRACERlab FXF-N合成仪自动化合成9-(4-18F-3-羟甲基丁基)鸟嘌呤(188F-FHBG).以N2-(对甲氧苯基二苯基甲基)-9-(4-甲苯磺酰基)-3-对甲氧苯基二苯基甲氧基-甲基丁基]鸟嘌呤为前体,在同一反应瓶中经亲核氟化、水解两步反应及SEP-PAK小柱分离纯化制备18 F-FHBG注射液,总合成时间<40 min,未校正放化产率为7%-12%(n>10),放化纯度>95%.用SEP-PAK分离纯化的一锅法,操作简便,很容易实现18F-FHBG的自动化合成.

关 键 词:酶报告基因  自动化合成

A simple and rapid automated synthesis of 18F-FHBG as a reporter gene expression PET imaging agent
TANG Ganghua,TANG Xiaolan,WANG Mingfang,LI Baoyuan,LIANG Mingquan,WANG Quanshi.A simple and rapid automated synthesis of 18F-FHBG as a reporter gene expression PET imaging agent[J].Nuclear Techniques,2009,32(8).
Authors:TANG Ganghua  TANG Xiaolan  WANG Mingfang  LI Baoyuan  LIANG Mingquan  WANG Quanshi
Abstract:Via one-pot procedure in a TRACERlab FXF-N synthesizer,the fully automated synthesis of 9-(4-18F]fluoro-3- hydroxymethylbutyl)guanine (18F-FHBG) as a reporter gene expression PET imaging agent is described in this paper.18F-FHBG was produced via two-step reactions including nucleophilic fluorination of the precursor molecule N2-monomethoxy trityl-9-(4-tosyl)-3-monomethoxytrityl-methylbutyl] guanine with 18F-fluoride and subsequent hydrolysis of the intermediate with protecting group with 1 mol/L HC1 at the same reaction vessel,and purification with SEP-PAK C18 cartridge.The decay-uncorrected radiochemical yield of 18F-FHBG was 7%-12% (n>10),with radiochemical purity of over 95%,and the total synthesis time was less than 40 min.One-pot synthesis procedure combined with SEP-PAK purification is easy to operate and can be used to fully automatedsynthesis of 18F-FHBG at an automated system such as a TRACERlab FXF-N synthesizer.
Keywords:18F-FHBG  Enzyme reporter gene  18F-FHBG  Automated synthesis
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