Simple and rapid synthesis of tumor imaging agents<sup>18</sup>F-FAC and <sup>18</sup>F- FMISO

TANG Ganghua TANG Xiaolan WANG Mingfang LUO Lei GAN Manquan

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Simple and rapid synthesis of tumor imaging agents¹⁸F-FAC and ¹⁸F- FMISO

更新时间：2021-03-12

- Simple and rapid synthesis of tumor imaging agents¹⁸F-FAC and ¹⁸F- FMISO
- NUCLEAR TECHNIQUES Issue 8, (2006)
- 作者机构：
  
  1. 南方医科大学南方医院核医学科PET中心
  2. 华南农业大学理学院
- 作者简介：
- 基金信息：
  
  广东省科技计划资助项目(2003C34304)
- DOI：
  CLC： R817
- Published：01 August 2006
- 稿件说明：
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[1]唐刚华,唐小兰,王明芳,罗磊,甘满权.简便、快速自动化合成肿瘤显像剂~(18)F-氟代乙酸盐和1-H-1-(3-~(18)F-2-羟基丙基)-2-~(18)F-硝基咪唑[J].核技术,2006(08):581-586.

TANG Ganghua TANG Xiaolan WANG Mingfang LUO Lei GAN Manquan. Simple and rapid synthesis of tumor imaging agents¹⁸F-FAC and ¹⁸F- FMISO[J]. Nuclear techniques, 2006, (8): 581-586.
[1]唐刚华,唐小兰,王明芳,罗磊,甘满权.简便、快速自动化合成肿瘤显像剂~(18)F-氟代乙酸盐和1-H-1-(3-~(18)F-2-羟基丙基)-2-~(18)F-硝基咪唑[J].核技术,2006(08):581-586. DOI：

TANG Ganghua TANG Xiaolan WANG Mingfang LUO Lei GAN Manquan. Simple and rapid synthesis of tumor imaging agents¹⁸F-FAC and ¹⁸F- FMISO[J]. Nuclear techniques, 2006, (8): 581-586. DOI：

摘要

用“一锅法”和TRACERlab FXF-N自动化合成仪系统合成了18F-氟代乙酸盐（18F-FAC）和1-H-1-（3-18F-2-羟基丙基）-2-硝基咪唑（18F-FMISO）。以溴代乙酸苄酯为前体

在同一反应瓶中经亲核氟化、NaOH水解两步反应及Sep Pak小柱分离纯化制备了18F-FAC注射液

总合成时间小于40min

未经校正的放化产率和放化纯度分别大于45％和99％。以1-（2’-硝基-1’-咪唑基）-2-O-四氢吡喃基-3-O-甲苯磺酰基丙二醇为原料

用类似方法制备了18F-FMISO注射液

总合成时间小于40 min

未经校正的放化产率和放化纯度分别大于40％和95％。采用“一锅法”自动化合成18F-FAC和18F-FMISO注射液

操作简便

该工艺可用制备2-18F-2-脱氧-D-葡萄糖（18F-FDG）的全自动化合成模块来制备18F-FAC和18F-FMISO注射液。

Abstract

The fully automated synthesis of tumor imaging agents 18F-fluoroacetate （18F-FAC） and 1-H-1-（3-[18F]fluoro-2-hydro-xylpropyl）-2-nitroimidazole （18F-FMISO） via "one-pot" procedure in TRACERlab FXF-N synthesizer is described. 18F-FAC injection was prepared via two-step reactions including nucleophilic fluorination of the precursor benzyl bromoacetate with 18F-fluoride and subsequently hydrolysis with NaOH at the same reaction vessel

and purified with Sep Pak cartridges. The uncorrected radiochemical yield of 18F-FAC was about 45%

the radiochemical purity was more than 99%

and the whole synthesis time was less than 40 min. 18F-FMISO injection was prepared by the similar method. The uncorrected radiochemical yield of 18F-FMISO is above 40%

the radiochemical purity is above 95%

and the total synthesis time was less than 40 min. The fully automated one-pot synthesis procedures of 18F-FAC and 18F-FMISO injection are easy to operate and can be performed in any automated system designed for the synthesis of 2-18F-2-deoxy-D-glucose （18F-FDG） by the nucleophilic substitution.

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Related Author

李葆元

王明芳

王全师

梁明泉

TANG Ganghua1 TANG Xiaolan2 WANG Mingfang1 LI Baoyuan1 LIANG Mingquan1 WANG Quanshi1 1

王明芳

甘满权

罗磊

Related Institution

PET Centre,Department of Nuclear Medicine,Nan Fang Hospital,Southern Medical University,Guangzhou 510515,China) 2

PET Centre, Department of Nuclear Medicine, Nan Fang Hospital, Southern Medical University, Guangzhou 510515) 2

南方医科大学南方医院核医学科PET中心

Department of Nuclear Medicine, Nanfang Hospital, Southern Medical University

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Simple and rapid synthesis of tumor imaging agents18F-FAC and 18F- FMISO

DOI：

摘要

Abstract

关键词

Keywords

references

Simple and rapid synthesis of tumor imaging agents¹⁸F-FAC and ¹⁸F- FMISO