文献类型：期刊文献

中文题名：心肌灌注显像剂^(99m)Tc-替曲膦的制备与应用

英文题名：Preparation and Application of Myocardial Perfusion Imaging Agent ^(99m)Tc-Tetrofosmin

作者：虞燕华[1];罗世能[1];沈永嘉[2];陈志明[1];汪洋[1]

机构：[1]江苏省原子医学研究所,无锡214063;[2]华东理工大学精细化工研究所,上海200237

年份：2006

卷号：32

期号：12

起止页码：1445

中文期刊名：华东理工大学学报（自然科学版）

外文期刊名：Journal of East China University of Science and Technology

收录：CSTPCD;;EI(收录号：20070710428107);Scopus;北大核心:【北大核心2004】；CSCD:【CSCD2011_2012】；

语种：中文

中文关键词：乙二膦;乙烯基乙醚;心肌灌注显像剂;双膦化舍物;^99mTc-替曲膦

外文关键词：1,2-bis （phosphino） ethane ; ethyl vinyl ether ; myocardial perfusion imaging agent ; bisphosphonate ; ^99mTc-tetrofosmin

摘要：亚磷酸三乙酯与1,2二-溴乙烷的加成产物经L iA lH4还原得乙二膦,后者与乙烯基乙醚发生加成反应生成1,2双-[双(2乙-氧基乙基)膦基]乙烷(替曲膦),这是一种新型的心肌灌注显像剂99mT c替-曲膦的配体,产物及中间产物经IR、1H-NMR、M S得到确证。用SnC l2将99mT cO-4还原成[99mT cO2]+后与替曲膦反应得到99mT c替-曲膦,其放射化学纯度为93%。临床使用表明:制得的99mT c替-曲膦能够满足临床显像要求,且标记简便。
Tetraethyl ethylenediphosphonate was synthezised by reaction of triethyl phosphite with 1,2 dibromoethane. It was reduced by lithium aluminum hydride to generate 1,2-Bis（phosphino）-ethane. 1,2-bis[-bis （2-ethoxyethyl）phosphino3 ethane （tetrofosmin） produced from the reaction of 1,2-bis （phosphino）- ethane with ethyl vinyl ether. Tetrofosmin is the ligand of ^99mTc-tetrofosmin, which is a novel myocardial perfusion imaging agent. Products of each reaction were characterized by IR, XH-NMR and MS. Tetrofosmin was radiolabelled by [^99mTcO2]^＋, obtained from the reaction of ^99mTcO4^- with SnCl2, to afford ^99mTc tetrofosmin, which met the requirements in the clinical trial.