A one-step synthesis of O-(2-[<sup>18</sup>F]fluoroethyl)-L-tyrosine via direct radiofluorination

WANG Mingwei YIN Duanzhi CHENG Dengfeng LI Gucai ZHENG Mingqiang ZHOU Wei WANG Yongxian

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A one-step synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine via direct radiofluorination

更新时间：2021-03-12

- A one-step synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine via direct radiofluorination
- NUCLEAR TECHNIQUES Issue 7, (2006)
- 作者机构：
  
  1. 中国科学院上海应用物理研究所放射性药物研究中心
  2. 中国科学院上海应用物理研究所放射性药物研究中心,上海,201800
- 作者简介：
- 基金信息：
  
  中国科学院知识创新工程重大资助项目(KJCX-SW-08);国家自然科学基金资助项目(30371634)
- DOI：
  CLC： O621.3;O644.2
- Published：01 July 2006
- 稿件说明：
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[1]王明伟,尹端沚,程登峰,李谷才,郑明强,周伟,汪勇先.直接亲核放射氟化法合成O-(2-[~(18)F]氟乙基)-L-酪氨酸[J].核技术,2006(07):522-526.

WANG Mingwei YIN Duanzhi CHENG Dengfeng LI Gucai ZHENG Mingqiang ZHOU Wei WANG Yongxian. A one-step synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine via direct radiofluorination[J]. Nuclear techniques, 2006, (7): 522-526.
[1]王明伟,尹端沚,程登峰,李谷才,郑明强,周伟,汪勇先.直接亲核放射氟化法合成O-(2-[~(18)F]氟乙基)-L-酪氨酸[J].核技术,2006(07):522-526. DOI：

WANG Mingwei YIN Duanzhi CHENG Dengfeng LI Gucai ZHENG Mingqiang ZHOU Wei WANG Yongxian. A one-step synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine via direct radiofluorination[J]. Nuclear techniques, 2006, (7): 522-526. DOI：

摘要

本文利用一种方便易得的前体N-叔丁氧羰基-（O-（2-对甲苯乙氧基））-L-酪氨酸甲酯

采用“一步法”直接亲核放射氟化法合成了O-（2-[18F]氟乙基）-L-酪氨酸。采用易于自动化的固相萃取法代替比较耗时的高压液相色层法分离目标产物

简化了制备过程

缩短了总合成时间。放射化学产率约为40%（未经衰变校正）

放射化学纯度大于97%

合成时间小于50min。

Abstract

O-(2-[18F]fluoroethyl)-L-tyrosine was synthesized via “one-step” method of nuclephilic radiofluorination with a precursor N-BOC-(O-2-tosyloxyethyl)-L-tyrosine methyl ester which is easy to obtain. Separation was per- formed on Sep-pak cartridge with solid phase extraction

instead of HPLC (high pressure liquid chromatography). The operation process was simple and the total synthesis time was less than 50 min. The radiochemical yield was about 40% (without decay-correction)

and the radiochemical purity was more than 97%.

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Related Author

Wenhui FAN

Hanzhou LIU

Wanxin WEN

WANG Mingwei YIN Duanzhi WANG Yongxian

尹端沚

汪勇先

Related Institution

School of Radiation Medicine and Protection, Medical College of Soochow University, Jiangsu Provincial Key Laboratory of Radiation Medicine and Protection

Radiopharmaceuticals Centre, Shanghai Institute of Applied Physics, the Chinese Academy of Sciences

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A one-step synthesis of O-(2-[18F]fluoroethyl)-L-tyrosine via direct radiofluorination

DOI：

摘要

Abstract

关键词

Keywords

references

A one-step synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine via direct radiofluorination