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

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

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（~７７Ｂｒ）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．

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.