3-正丁基锡-N-琥珀酰亚胺苯甲酸酯的合成及其~(125)I标记

Synthesis and ~(125)I Labeling of N-Succinimidyl-3-(tri-n-butylstannyl)benzoate

摘要: 合成了3-正丁基锡-N-琥珀酰亚胺苯甲酸酯(ATE)和N-琥珀酰亚胺-3-碘苯甲酸酯(SIB),其产率分别为45.4%和71.4%,并用核磁、质谱、红外等对它们的结构进行了表征。对ATE进行了125I标记,得到S125IB,标记率可达93.0%,放化纯度>98.0%。本方法为放射性药物碘的间接标记提供了重要参考。

Abstract: N-succinimidyl-3-(tri-n-butylstannyl)benzoate(ATE) and N-succinimidyl-3-iodobenzoate(SIB) is synthesized.The structures of ATE and SIB are confirmed with ~1HNMR,MS and IR.The yields of ATE and SIB are 45.4% and 71.4%,respectively.ATE is labeled with ~(125)I.The labeling field is 93.0% and radiochemical purity is over 98.0%.The synthesis and the labeling of ATE has a important value for indirect label of radiopharmaceuticals.