3-三甲基硅苄胍的合成及其<sup>125</sup>I标记

3-三甲基硅苄胍的合成及其¹²⁵I标记

摘要: 以3-溴甲苯为起始物，通过5步反应合成可用于放射性碘（砹）标记的3-三甲基硅苄胍，并用核磁共振（NMR）、质谱（MS）、高效液相（HPLC）等对产物进行了表征。以此化合物为前体，对其进行了¹²⁵I标记。¹²⁵I MIBG的标记率达66.7%，放化纯度＞98%。标记物在室温下放置3 d后，放化纯度无明显变化，表明¹²⁵I MIBG具有较高的体外稳定性。

Abstract: 3-trimethylsilylbenzylguanidine, a precursor for ^125,131IMIBG or ²¹¹At MABG was synthesized in five steps using 3-bromotoluene as starting materials, and was characterized by NMR, MS and HPLC. With this precursor, free-carrier 125IMIBG was obtained with a labeling yield of 66.7% and radiochemical purity of more than 98% after purified using HPLC. Even stayed for 3 d at room temperature, the ¹²⁵I-MIBG maintains constantly stable in vitro, with radiochemical purity of more than 95%.