Synthesis and fluoro-radiolabelling of dopamine D<sub>2</sub> receptor imaging agent <sup>18</sup>F-FSABZM

CHEN Jian1 ZHANG Zhengwei2 GUAN Yihui2 ZHU Jianhua1 1

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Synthesis and fluoro-radiolabelling of dopamine D₂ receptor imaging agent ¹⁸F-FSABZM

更新时间：2021-03-12

- Synthesis and fluoro-radiolabelling of dopamine D₂ receptor imaging agent ¹⁸F-FSABZM
- NUCLEAR TECHNIQUES Issue 5, (2006)
- 作者机构：
  
  1. 复旦大学药学院放射药学教研室
  2. 复旦大学华山医院核医学科PET中心
  3. 复旦大学药学院放射药学教研室,上海,200032
  4. ,上海,200040
- 作者简介：
- 基金信息：
- DOI：
  CLC： TQ421.7
- Published：01 May 2006
- 稿件说明：
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[1]陈键,张政伟,管一晖,朱建华.苯甲酰胺类多巴胺D_2受体显像剂~(18)F-FSABZM的合成和标记[J].核技术,2006(05):354-357.

CHEN Jian1 ZHANG Zhengwei2 GUAN Yihui2 ZHU Jianhua1 1. Synthesis and fluoro-radiolabelling of dopamine D₂ receptor imaging agent ¹⁸F-FSABZM[J]. Nuclear techniques, 2006, (5): 354-357.
[1]陈键,张政伟,管一晖,朱建华.苯甲酰胺类多巴胺D_2受体显像剂~(18)F-FSABZM的合成和标记[J].核技术,2006(05):354-357. DOI：

CHEN Jian1 ZHANG Zhengwei2 GUAN Yihui2 ZHU Jianhua1 1. Synthesis and fluoro-radiolabelling of dopamine D₂ receptor imaging agent ¹⁸F-FSABZM[J]. Nuclear techniques, 2006, (5): 354-357. DOI：

摘要

将5-硝基取代苯甲酰胺类化合物经硝基还原、N-双羟乙基化、甲磺酰化等反应制备氟标记前体

用K222催化进行氟标记

合成了（S）-N-[（1-乙基-2-吡咯烷基）甲基]-5-[N-（2-[18F]氟乙基）-N-甲基磺酰基]胺基-2-甲氧基苯甲酰胺（（S）-N-[（1-ethyl-2-pyrrolidinyl）methyl]-5-[N-（2-[18F]fluoroethyl）-N-methylsulfonyl]amino-2-methoxy-ben-zamide

18F-FSABZM）。标记前体、冷标记产物和各步合成中间体均经过核磁共振和质谱确证。结果显示

经HPLC检测

标记率为12%—15%

合成及纯化时间80—90min

纯化后放化纯度大于97%

稳定性好。

Abstract

The preparation of a 18F-labeled imaging agent with higher affinity to dopamine D2 receptor is reported. The ligand of (S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5- [N-(2-[18F]fluoroethyl)-N-methylsulfonyl]amino-2- methoxybenzamide (18F-FSABZM) was synthesized by nitryl reduction

N-dihydroxyethylation

and methylsulfon- ylation. Finally

18F-FSABZM was prepared by nucleophilic fluorination of the mesylate with K18F/K222(Kryptofix). The chemical structure of the fluoro-labeling precursor SABZM

the labeling product with non-radioactive fluorine and all other intermediates were validated by 1HNMR and MS. Determined by HPLC

the labeling yield was 12%— 15%. After purifying

the resultant 18F-FSABZM

with a radiochemical purity of over 97%

was stable for more than 4 hours at room temperature. The whole process (including synthesis and analysis) took only 80—90 minutes.

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Synthesis and fluoro-radiolabelling of dopamine D2 receptor imaging agent 18F-FSABZM

DOI：

摘要

Abstract

关键词

Keywords

references

Synthesis and fluoro-radiolabelling of dopamine D₂ receptor imaging agent ¹⁸F-FSABZM