Sogbein Oyebola O, Green Andrew E C, Valliant John F
Department of Chemistry, McMaster University, Hamilton, Ontario, Canada L8S 4M1.
Inorg Chem. 2005 Dec 12;44(25):9585-91. doi: 10.1021/ic051123t.
A method for the preparation of eta5-metallocarborane complexes of technetium-99m in water was developed. The key to the procedure is the use of aqueous sodium or potassium fluoride, which prevents premature degradation of the Tc(I) starting material used to prepare the carborane complexes. Solid-phase extraction was used to purify Tc-metallocarboranes derived from both ortho and meta isomers, which were isolated in good to excellent yields in high radiochemical purities. In conjunction with these studies, a series of fluoride-based "kits" were developed to produce the key precursor [99mTc(CO)3(H2O)3]+ in the absence of any other stabilizing ligand. Using this approach, [99mTc(CO)3(H2O)3]+ could be prepared directly from 99mTcO4- under a range of pH values, including neutral pH, which affords the opportunity to develop one-pot labeling procedures for base-sensitive targeting vectors.
开发了一种在水中制备锝-99m的η5-金属碳硼烷配合物的方法。该方法的关键在于使用氟化钠或氟化钾水溶液，这可防止用于制备碳硼烷配合物的Tc（I）起始原料过早降解。采用固相萃取法纯化源自邻位和间位异构体的锝-金属碳硼烷，其分离产率良好至优异，放射化学纯度高。结合这些研究，开发了一系列基于氟化物的“试剂盒”，以在不存在任何其他稳定配体的情况下制备关键前体[99mTc(CO)3(H2O)3]+。采用这种方法，[99mTc(CO)3(H2O)3]+可在包括中性pH在内的一系列pH值下直接由99mTcO4-制备，这为开发针对碱敏感靶向载体的一锅法标记程序提供了机会。
