Synthesis of precursor and radiolabelling of neuroreceptor imaging agent ￣（77）Br-p-bromospiroperidol

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Synthesis of precursor and radiolabelling of neuroreceptor imaging agent ￣（77）Br-p-bromospiroperidol

更新时间：2021-04-09

- Synthesis of precursor and radiolabelling of neuroreceptor imaging agent ￣（77）Br-p-bromospiroperidol
- NUCLEAR TECHNIQUES Issue 4, (1994)
- 作者机构：
  
  1. 中国科学院上海原子核研究所
  2. 都市卫生防疫站
- 作者简介：
- 基金信息：
- DOI：
  CLC： TQ572
- Published：01 April 1994
- 稿件说明：
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[1]黄永学,李永键.神经受体显像剂溴（~（77）Br）代螺环哌啶醇前体合成及放射性标记研究[J].核技术,1994(04):233-237.

Synthesis of precursor and radiolabelling of neuroreceptor imaging agent ￣（77）Br-p-bromospiroperidol[J]. Nuclear techniques, 1994, (4).
[1]黄永学,李永键.神经受体显像剂溴（~（77）Br）代螺环哌啶醇前体合成及放射性标记研究[J].核技术,1994(04):233-237. DOI：

Synthesis of precursor and radiolabelling of neuroreceptor imaging agent ￣（77）Br-p-bromospiroperidol[J]. Nuclear techniques, 1994, (4). DOI：

摘要

完成了一种七步化学合成得到前体螺环哌啶醇的方法，并用Ｈ２Ｏ２－冰醋酸氧化标记法和ＴＬＣ纸层析法分离合成了溴（

７

７Ｂｒ）代螺环哌啶醇。标记率为９２％，放射化学产率为７８％，产品的放射化学纯度＞９５％。并对该放射性药物在小白鼠脑内的吸收分布作了初步研究，结果表明在大脑纹状体中的摄取率可高出小脑６倍．

Abstract

his report describes the routine method for producing spiroperidol by seven steps of chemical synthesis. Br-p-bromospiroperidol was prepared by reacting 77Br

H2O2 and spiroperidol in glacial acetic acid. The purity of the product was checked by TLC. The labelling rate was 92% and the overall radiochemical yield was 78% with radiochemical purity of 95%. The in vivo distribution of 77Br-p-bromospiroperidol in the mouse brain was studied. It was shown that the uptake of 77Br-p-bromospiroperidol in striatum was six times higher than that in cerebellum.

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