用于放射性核素铼标记的fac-[^(188)Re(CO)_3(H_2O)_3]^+的制备研究

Preparation of fac-[^(188)Re(CO)_3(H_2O)_3]^+ for Labeling of Radionuclide Rhenium

目的:探讨放化中间体fac-[188Re(CO)3(H2O)3]+的合成条件,并对其进行优化研究。方法:参照Schibli介绍的方法进行放化中间体fac-[188Re(CO)3(H2O)3]+的合成,分别从反应温度、反应时间和反应物BH3.NH3的用量对合成fac-[188Re(CO)3(H2O)3]+产率的影响进行观察。结果:合成放化中间体fac-[188Re(CO)3(H2O)3]+的最佳反应条件为:反应时间为15min,反应温度为70℃,BH3.NH3的用量为5mg;pH值<2。在最佳的反应条件下,产物的放化产率为85%,经Sep-Pak(硅胶柱分离后,放化纯度>95%。结论:本文结果为放化中间体fac-[188Re(CO)3(H2O)3]+标记生物分子作为新一代治疗药物的发展提供了有力的实验基础。

Objective To investigate the optimal synthesizing conditions of intermediate fac-[188Re（CO）3（H2O）3]＋.Methods The complex of fac-[188Re（CO）3（H2O）3]＋ was synthesized according to the method reported by Schibli.The effects of reaction temperature,reaction time,and the amount of BH3·NH3 on yields of fac-[188Re（CO）3（H2O）3]＋ were studied.Results The optimal reactive condition was：15min of reaction time,70℃ of reaction temperature and 5mg of BH3·NH3 at pH2.Overall radiochemical yield of 85% was obtained at optimal condition,and a radiochemical purity of over 95% after a Sep-Pak silica cartridge separation was reached.Conclusion The research results may sapport the application of fac-[188Re（CO）3（H2O）3]＋ as a potential ideal candidate agent for labeling biomolecules.