Automated synthesis of <sup>18</sup>F-fluorothymidine via Sep-Pak purification

WEN Fuhua DENG Huaifu TANG Ganghua YI Chang WU Kening

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Automated synthesis of ¹⁸F-fluorothymidine via Sep-Pak purification

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- Automated synthesis of ¹⁸F-fluorothymidine via Sep-Pak purification
- NUCLEAR TECHNIQUES Vol. 33, Issue 8, (2010)
- 作者机构：
  
  中山大学附属第一医院核医学科PET-CT
- 作者简介：
- 基金信息：
  
  国际原子能机构(IAEA)资助(15245);中山大学“百人计划”引进人才科研启动基金(80000-3126132);国家高技术研究发展计划(863计划)专题(2008AA02Z430)
- DOI：
  CLC： R817
- Published：01 August 2010
- 稿件说明：
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[1]文富华,邓怀福,唐刚华,易畅,吴克宁.柱分离法自动化合成~(18)F-FLT[J].核技术,2010,33(08):598-602.

WEN Fuhua DENG Huaifu TANG Ganghua YI Chang WU Kening. Automated synthesis of ¹⁸F-fluorothymidine via Sep-Pak purification[J]. Nuclear techniques, 2010, 33(8): 598-602.
[1]文富华,邓怀福,唐刚华,易畅,吴克宁.柱分离法自动化合成~(18)F-FLT[J].核技术,2010,33(08):598-602. DOI：

WEN Fuhua DENG Huaifu TANG Ganghua YI Chang WU Kening. Automated synthesis of ¹⁸F-fluorothymidine via Sep-Pak purification[J]. Nuclear techniques, 2010, 33(8): 598-602. DOI：

摘要

使用PET-MF-2V-IT-I型氟-18多功能合成模块

以3-N-t-叔丁氧羰基-1-[5’-O-（4

4’-二甲氧基三苯甲基）-2’-脱氧-3’-O-（4-硝基苯磺酰基-β-1）-苏戊呋喃糖]胸腺嘧啶为前体

经氟化、水解后小柱分离制得18F-FLT注射液。对荷肝细胞癌小鼠进行18F-FLTPET/CT显像

结果显示

柱分离法合成18F-FLT耗时～35min

放化产率为12%-15%

放化纯度>95%。表明18F-FLT静脉注射1h后肿瘤对18F-FLT的摄取明显高于周围正常组织。该法合成简单、反应时间短、产率高

可满足临床应用。

Abstract

A fully automated synthesis of 18F-flurorthymidine(18F-FLT) was performed on PET-MF-2V-IT-I system.18F-FLT was obtained via two-step reactions

including nucleophilic fluorination of 3-N-t-butoxycarbonyl-1-[5’-O-(4

4’-di-methoxytriphenylmethyl)-2’-deoxy-3’-O-(4-nitrobenzenesulfonyl)-β-D-threopentofuranosy]thymine with fluoride

and subsequent hydrolysis of the protecting group with HCl in the same reaction vessel and purification with three Sep-Paks.18F-FLT PET/CT images were performed on mice models bearing hepatocellular carcinoma.Fully automated synthesis of 18F-FLT was completed within the total synthesis time of about 35 min.The uncorrected radiochemical yield was between 12% and 15%

the radiochemical purity was over 95%.The quality control indexes of 18F-FLT injection met the requirements of radiopharmaceuticals quality.18F-FLT PEC/CT imaging showed high uptake in the tumors.This method provides simple and rapid synthesis of 18F-FLT with short radiosynthesis time and a high radiochemical yield for clinical need.

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Related Institution

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Automated synthesis of 18F-fluorothymidine via Sep-Pak purification

DOI：

摘要

Abstract

关键词

Keywords

references

Automated synthesis of ¹⁸F-fluorothymidine via Sep-Pak purification