Routinely automated production of 3’-deoxy-3’-[<sup>18</sup>F] fluorothymidine as a specific molecular imaging probe of tumor cell proliferation

WANG Mingwei ZHANG Yingjian ZHANG Yongping

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Routinely automated production of 3’-deoxy-3’-[¹⁸F] fluorothymidine as a specific molecular imaging probe of tumor cell proliferation

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- Routinely automated production of 3’-deoxy-3’-[¹⁸F] fluorothymidine as a specific molecular imaging probe of tumor cell proliferation
- NUCLEAR TECHNIQUES Vol. 34, Issue 7, (2011)
- 作者机构：
  
  1. 复旦大学附属肿瘤医院核医学科
  2. 复旦大学上海医学院肿瘤学系
- 作者简介：
- 基金信息：
  
  国家自然科学基金(30700188);上海市科委重点科技支撑计划(08411954200)资助
- DOI：
  CLC： R817
- Published：01 July 2011
- 稿件说明：
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[1]王明伟,章英剑,张勇平.肿瘤细胞增殖特异性分子影像探针3'-脱氧-3'-[~(18)F]氟胸苷的自动化生产[J].核技术,2011,34(07):537-542.

WANG Mingwei ZHANG Yingjian ZHANG Yongping. Routinely automated production of 3’-deoxy-3’-[¹⁸F] fluorothymidine as a specific molecular imaging probe of tumor cell proliferation[J]. Nuclear techniques, 2011, 34(7): 537-542.
[1]王明伟,章英剑,张勇平.肿瘤细胞增殖特异性分子影像探针3'-脱氧-3'-[~(18)F]氟胸苷的自动化生产[J].核技术,2011,34(07):537-542. DOI：

WANG Mingwei ZHANG Yingjian ZHANG Yongping. Routinely automated production of 3’-deoxy-3’-[¹⁸F] fluorothymidine as a specific molecular imaging probe of tumor cell proliferation[J]. Nuclear techniques, 2011, 34(7): 537-542. DOI：

摘要

采用升级改进的Explora GN模块和半制备型HPLC分离纯化单元

基于"一锅-两步"法发展肿瘤细胞增殖特异性分子影像探针3’-脱氧-3’-[18F]氟胸苷（18F-FLT）的自动化生产方法:第一步是前体BDNT与活化18F离子之间的亲核放射[18F]氟化反应

120°C加热回流5 min

产生标记中间体18F-BDFT;第二步是18F-BDFT的水解反应

直接加入盐酸溶液

110°C加热5 min

生成目标产物18F-FLT

使用HPLC分离纯化。该18F-FLT自动化生产方法具备快速、可靠和连续多次合成能力的特点

总合成时间小于65 min

放射化学产率为15%-25%（未衰减校正

n>20）。18F-FLT所有质量控制指标都符合放射性药物的质量要求

其中放射化学纯度大于99%、化学纯度和比活度均很高。

Abstract

This work was aimed at developing a routine for automated production of 3’-deoxy-3’-[18F]fluorothymidine(18F-FLT)

a specific molecular imaging probe of tumor cell proliferation

using one-pot two-step strategy and an upgraded Explora GN module integrated with a semi-preparative HPLC system.Firstly

the nucleophilic [18F]radiofluorination of precursor BDNT with activated 18F ion was carried out at 120°C for 5 min to yield the labeled intermediate 18F-BDFT.Secondly

the acidic hydrolysis of 18F-BDFT was run at 110°C for 5 min to produce 18F-FLT after addition of HCl

and 18F-FLT was purified by HPLC.This automated production of 18F-FLT is of fast

reliable and multi-run features

being completed within 65 min with radiochemical yield of 15%-25%(without decay correction).The quality control of 18F-FLT was identical with the radiopharmaceutical requirements

especiallly the radiochemical purity of greater than 99% and high chemical purity and specific activity own to HPLC purification.

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Routinely automated production of 3’-deoxy-3’-[18F] fluorothymidine as a specific molecular imaging probe of tumor cell proliferation

DOI：

摘要

Abstract

关键词

Keywords

references

Routinely automated production of 3’-deoxy-3’-[¹⁸F] fluorothymidine as a specific molecular imaging probe of tumor cell proliferation