Synthesis of N-succinimidyl-4-[<sup>18</sup>F]fluorobenzoate

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

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Synthesis of N-succinimidyl-4-[¹⁸F]fluorobenzoate

更新时间：2021-03-12

- Synthesis of N-succinimidyl-4-[¹⁸F]fluorobenzoate
- NUCLEAR TECHNIQUES Issue 12, (2006)
- 作者机构：
  
  1. 中国科学院上海应用物理研究所放药中心
  2. 中国科学院上海应用物理研究所放药中心,上海,201800
- 作者简介：
- 基金信息：
  
  中国科学院知识创新工程重大项目(KJCX-SW-08);国家自然科学基金(30371634)资助
- DOI：
  CLC： TQ463.2
- Published：01 December 2006
- 稿件说明：
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[1]程登峰,尹端沚,王明伟,李谷才,周伟,汪勇先.N-琥珀酰亚胺4-[~(18)F]氟苯甲酸酯的合成[J].核技术,2006(12):917-920.

CHENG Dengfeng YIN Duanzhi WANG Mingwei LI Gucai ZHOU Wei WANG Yongxian. Synthesis of N-succinimidyl-4-[¹⁸F]fluorobenzoate[J]. Nuclear techniques, 2006, (12): 917-920.
[1]程登峰,尹端沚,王明伟,李谷才,周伟,汪勇先.N-琥珀酰亚胺4-[~(18)F]氟苯甲酸酯的合成[J].核技术,2006(12):917-920. DOI：

CHENG Dengfeng YIN Duanzhi WANG Mingwei LI Gucai ZHOU Wei WANG Yongxian. Synthesis of N-succinimidyl-4-[¹⁸F]fluorobenzoate[J]. Nuclear techniques, 2006, (12): 917-920. DOI：

摘要

合成了18F标记多肽和蛋白类药物中常用的中间体N-琥珀酰亚胺-4-[18F]氟苯甲酸酯（[18F]SFB）。由于[18F]SFB能和生物分子结合达到较高的标记率以及具有较好的体内稳定性

成为一种最适宜的氟-18标记试剂。本工作首先合成标记前体乙基-4-三甲胺苯甲酸酯-三氟磺酸盐

接下来经三步放射合成

然后经Sep-PakC18柱分离可得[18F]SFB

并对第一步的18F标记反应进行了优化。合成时间约1h;放化产率约50%;经放射性TLC和HPLC分析

放化纯度大于98%。

Abstract

We have synthesized 18F–labeled prosthetic group

N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) for fluorine-18 labeling peptides and proteins. [18F]SFB seems to be the most suitable 18F-labeling agent because of its higher labeling yield and better stability of the conjugates in vivo. Labeling prosthetic group

triflate salt of ethyl p-trimethylammonium benzoate

was synthesized first

then the radio-synthesis with three steps was carried out

and the first step about 18F –labeling was optimized. After purifying through Sep-Pak C18 cartridge

[18F]SFB was produced with the decay-corrected radiochemical yield of 50% within 1 hour.The radiochemical purity was more than 98% by using radio-TLC and HPLC.

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Related Author

张岚

汪勇先

周伟

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WANG Mingwei YIN Duanzhi WANG Yongxian

尹端沚

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中国科学院研究生院

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

中国科学院上海应用物理研究所放射性药物研究中心

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Synthesis of N-succinimidyl-4-[18F]fluorobenzoate

DOI：

摘要

Abstract

关键词

Keywords

references

Synthesis of N-succinimidyl-4-[¹⁸F]fluorobenzoate