Abstract DATA (6-Amino-1,4-diazapine-triacetate) and AAZTA (6-Amino-1,4-diazapine-tetracetate) chelators represent a novel approach representing hybrid-chelates: possessing significant cyclic and acyclic character. It is believed that flexibility of the acyclic part facilitates rapid complexation, whilst the preorganized cyclic part minimizes the energy barrier to complexation and inhibits decomplexation processes. So far, these chelators have been used exclusively with 44Sc and 68Ga only. Recent results with natCu predict high stabilities for Cu-AAZTA, yet no radioactive labeling of AAZTA or DATA with 64Cu or any additional radioactive isotope has been reported. We present the one pot synthesis of the bifunctional derivatives AAZTA5OMe and DATA5mOMe and their labeling with 64Cu. In addition, in vitro stability of the respective complexes are presented.

中文翻译：

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温和高效的 64Cu 标记过氢-1, 4-二氮杂衍生物，可用于大肽、蛋白质和抗体

摘要 DATA（6-Amino-1,4-diazapine-triacetate）和AAZTA（6-Amino-1,4-diazapine-tetracetate）螯合剂代表了一种代表混合螯合物的新方法：具有显着的环状和非环状特征。据信，无环部分的柔韧性有利于快速络合，而预先组织的环状部分使络合的能量障碍最小化并抑制解络过程。到目前为止，这些螯合剂仅用于 44Sc 和 68Ga。最近使用 natCu 的结果预测 Cu-AAZTA 具有高稳定性，但尚未报道使用 64Cu 或任何其他放射性同位素对 AAZTA 或 DATA 进行放射性标记。我们展示了双功能衍生物 AAZTA5OMe 和 DATA5mOMe 的一锅合成及其用 64Cu 标记。此外，