Radiochemical synthesis of O-(2-[<sup>18</sup>F]fluoroethyl)-L-tyrosine as PET imaging agent for tumor diagnosis

WANG Mingwei1; 2 YIN Duanzhi WANG Yongxian LI Junling ZHAN Lan ZHOU Wei 1

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Radiochemical synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine as PET imaging agent for tumor diagnosis

更新时间：2021-03-12

- Radiochemical synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine as PET imaging agent for tumor diagnosis
- NUCLEAR TECHNIQUES Issue 9, (2005)
- 作者机构：
  
  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 中国科学院研究生院北京,100049
- 作者简介：
- 基金信息：
  
  中科院知识创新工程重大项目资助(KJCX-SW-08)
- DOI：
  CLC： TQ421.7
- Published：01 September 2005
- 稿件说明：
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[1]王明伟,尹端沚,,,,,,,,,汪勇先,,,,,,,,,李俊玲,,,,,,,,,张岚,,,,,,,,,周伟.肿瘤PET显像剂O-(2-[~(18)F]氟乙基)-L-酪氨酸的放射化学合成[J].核技术,2005(09):654-658.

WANG Mingwei1, 2 YIN Duanzhi WANG Yongxian LI Junling ZHAN Lan ZHOU Wei 1. Radiochemical synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine as PET imaging agent for tumor diagnosis[J]. Nuclear techniques, 2005, (9): 654-658.
[1]王明伟,尹端沚,,,,,,,,,汪勇先,,,,,,,,,李俊玲,,,,,,,,,张岚,,,,,,,,,周伟.肿瘤PET显像剂O-(2-[~(18)F]氟乙基)-L-酪氨酸的放射化学合成[J].核技术,2005(09):654-658. DOI：

WANG Mingwei1, 2 YIN Duanzhi WANG Yongxian LI Junling ZHAN Lan ZHOU Wei 1. Radiochemical synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine as PET imaging agent for tumor diagnosis[J]. Nuclear techniques, 2005, (9): 654-658. DOI：

摘要

放射性核素标记的氨基酸近年来已成为放射性药物领域的研究热点。O-（2-[18F]氟乙基）-L-酪氨酸([

F]FET)从问世以来一直备受关注

是一种很有希望的脑肿瘤PET显像剂。本文选择“两步法”合成了[18F]

FET。首先

通过1

2-二对甲苯磺酸基乙烷的[18F]氟化制备标记中间体

即烷基化试剂2-[18F]

氟乙基对甲苯磺酸酯;然后

L-酪氨酸的[18F]氟乙基化合成了目标化合物[18F]

FET。总合成时间约为50min

放射化学产率为20%—30%（未经衰变校正）

放射化学纯度大于98%。

Abstract

Radiolabelled amino acids have been the interesting field of radiopharmaceuticals for several years

of which O-(2-[18F]fluoroethyl)-L-tyrosine is very promising as PET imaging agent for tumor diagnosis. [18F]FET was synthesized via a two-step reaction consisting of [18F]fluorination of 1

2-bis(tosyloxy)ethane for preparing the alkylating agent 2-[18F]fluoroethyltosylate and [18F]fluoroethylation of L-tyrosine for obtaining the objective [18F]FET. The synthesis was typically finished in less than 50 min with overall radiochemical yields of 20%—30% (without decay correction)and radiochemical purity more than 98%.

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Radiochemical synthesis of O-(2-[18F]fluoroethyl)-L-tyrosine as PET imaging agent for tumor diagnosis

DOI：

摘要

Abstract

关键词

Keywords

references

Radiochemical synthesis of O-(2-[¹⁸F]fluoroethyl)-L-tyrosine as PET imaging agent for tumor diagnosis