Vaidyanathan Ganesan, Zalutsky Michael R
Department of Radiology, Box 3808, Duke University Medical Center, Durham, North Carolina 27710, USA.
Nat Protoc. 2006;1(2):707-13. doi: 10.1038/nprot.2006.99.
A procedure for the synthesis of N-succinimidyl 3-iodobenzoate labeled with any iodine isotope ([*I]SIB), which is an agent used in the radioiodination of proteins and peptides, from its tin precursor N-succinimidyl 3-(tri-n-butylstannyl)benzoate (STB) is described. Also included are protocols for the synthesis of an unlabeled standard of SIB and the tin precursor. Radioiododestannylation of STB using tert-butylhydroperoxide as the oxidant gives [*I]SIB in 80% radiochemical yields. The total time for the synthesis of [*I]SIB from STB is approximately 95 min. Use of [*I]SIB yields radioiodinated proteins that are considerably more stable in vivo than those radioiodinated by the direct electrophilic method.
描述了一种从其锡前体N-琥珀酰亚胺基3-(三正丁基锡基)苯甲酸酯(STB)合成用任何碘同位素标记的N-琥珀酰亚胺基3-碘苯甲酸酯([*I]SIB)的方法，[*I]SIB是一种用于蛋白质和肽放射性碘化的试剂。还包括未标记的SIB标准品和锡前体的合成方案。以叔丁基过氧化氢为氧化剂对STB进行放射性碘脱锡反应，得到放射性化学产率为80%的[*I]SIB。从STB合成[*I]SIB的总时间约为95分钟。使用[*I]SIB产生的放射性碘化蛋白质在体内比通过直接亲电方法放射性碘化的蛋白质稳定得多。
