4-甲基咪唑双膦酸的合成及其^(99)Tc^m标记

Synthesis of M_4IDP and Optimum Labeling Conditions of ^(99)Tc^m-M_4IDP

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。

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.