A simple and rapid automated synthesis of <sup>18</sup>F-FHBG as a reporter gene expression PET imaging agent

TANG Ganghua1; 2 TANG Xiaolan3 WANG Mingfang2 LI Baoyuan2 LIANG Mingquan2 WANG Quanshi21

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A simple and rapid automated synthesis of ¹⁸F-FHBG as a reporter gene expression PET imaging agent

更新时间：2021-03-12

- A simple and rapid automated synthesis of ¹⁸F-FHBG as a reporter gene expression PET imaging agent
- NUCLEAR TECHNIQUES Vol. 32, Issue 8, (2009)
- 作者机构：
  
  1. 中山大学附属第一医院核医学科PET-CT中心
  2. 南方医科大学南方医院核医学科PET中心
  3. 华南农业大学理学院
- 作者简介：
- 基金信息：
  
  中山大学“百人计划”引进人才科研启动基金(80000-3171313);国家高技术研究发展计划(863计划)专题课题(2008AA02Z430)
- DOI：
  CLC： R817.4
- Published：01 August 2009
- 稿件说明：
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[1]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~(18)F-FHBG[J].核技术,2009,32(08):609-613.

TANG Ganghua1, 2 TANG Xiaolan3 WANG Mingfang2 LI Baoyuan2 LIANG Mingquan2 WANG Quanshi21. A simple and rapid automated synthesis of ¹⁸F-FHBG as a reporter gene expression PET imaging agent[J]. Nuclear techniques, 2009, 32(8): 609-613.
[1]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~(18)F-FHBG[J].核技术,2009,32(08):609-613. DOI：

TANG Ganghua1, 2 TANG Xiaolan3 WANG Mingfang2 LI Baoyuan2 LIANG Mingquan2 WANG Quanshi21. A simple and rapid automated synthesis of ¹⁸F-FHBG as a reporter gene expression PET imaging agent[J]. Nuclear techniques, 2009, 32(8): 609-613. DOI：

摘要

用一锅法和TRACERlabFXF-N合成仪自动化合成9-（4-18F-3-羟甲基丁基）鸟嘌呤（18F-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18F-FHBG注射液

总合成时间<40min

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。

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 HCl 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 automated synthesis of 18F-FHBG at an automated system such as a TRACERlab FXF-N synthesizer.

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Related Author

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Related Institution

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PET-CT Center,Department of Nuclear Medicine,The First Affiliated Hospital,Sun Yat-Sen University

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A simple and rapid automated synthesis of 18F-FHBG as a reporter gene expression PET imaging agent

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摘要

Abstract

关键词

Keywords

references

A simple and rapid automated synthesis of ¹⁸F-FHBG as a reporter gene expression PET imaging agent