| 4-甲基咪唑双膦酸的合成及其~(99)Tc~m标记 |
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| 引用本文： | 翟好真,罗世能,王燕,邱玲,林建国,夏咏梅.4-甲基咪唑双膦酸的合成及其~(99)Tc~m标记[J].同位素,2010,23(4):225-229. |
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| 作者姓名： | 翟好真 罗世能 王燕 邱玲 林建国 夏咏梅 |
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| 作者单位： | [1]江南大学化学与材料工程学院,江苏无锡214122 [2]江苏省原子医学研究所,卫生部核医学重点实验室,江苏省分子核医学重点实验室,江苏无锡214063 |
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| 基金项目： | 国家自然科学基金资助项目，江苏省自然科学基金资助项目，吴阶平医学基金资助 |
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| 摘 要： | 以4-甲基咪唑为原料,通过N-烷基化、酯水解和磷酸酰化三步反应,合成1-羟基-2-(4-甲基-1H-咪唑基)-乙烷-1,1-双膦酸(M4IDP),目标产物和重要中间体通过IR、MS及1H NMR进行结构鉴定;采用Na99TcmO4标记M4IDP,得到标记物99Tcm-M4IDP,并测定其体外稳定性。结果显示,标记物的最佳标记条件为:反应时间30 min,反应体系pH为6,SnCl2.2H2O用量100μg,配体用量5 mg。在此条件下,标记率95%,室温下存放6 h,放化纯度95%,说明99Tcm-M4IDP具有较好的体外稳定性。
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| 关 键 词： | 99Tcm 标记 双膦酸 M4IDP |
Synthesis of M4IDP and Optimum Labeling Conditions of 99Tcm-M4IDP |
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| ZHAI Hao-zhen,LUO Shi-neng,WANG Yan,QIU Ling,LIN Jian-guo,XIA Yong-mei.Synthesis of M4IDP and Optimum Labeling Conditions of 99Tcm-M4IDP[J].Isotopes,2010,23(4):225-229. |
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| Authors: | ZHAI Hao-zhen LUO Shi-neng WANG Yan QIU Ling LIN Jian-guo XIA Yong-mei |
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| Affiliation: | 1.College of Chemical and Material Engineering, Jiangnan University, Wuxi 214122，China；2.Jiangsu Institute of Nuclear Medicine; Key Laboratory of Nuclear Medicine, Ministry of Health;Jiangsu Key Laboratory of Molecular Nuclear Medicine， Wuxi 214063，China |
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| Abstract: | 1-Hydroxy-2-（4-methyl-1H-imidazoleyl）-ethylidene-1,1-bisphosphonic（M4IDP）was prepared by three steps of N-alkylation、ester hydrolation and phosphoric acid acylation from the raw material 4-methyl-1H-imidazole.The structures of intermediate and target compounds were identified by Elemental Analysis、IR、MS and ^1H NMR.Then M4IDP was directly labeled by Na^99Tc^mO4 to afford ^99Tc^m-M4IDP.The results showed that the best labeling conditions were 30 minutes reaction time,pH 6,100 μg SnCl2·2H2O,and 5 mg M4IDP.In this condition,the labeling yield was more than 95% and ^99Tc^m-M4IDP showed good biological stability in vitro. |
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| Keywords: | ^99Tcm labeling bisphosphonic M4IDP |
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