Garg P K, Archer G E, Bigner D D, Zalutsky M R
Department of Radiology, Duke University Medical Center, Durham, NC 27710.
Int J Rad Appl Instrum A. 1989;40(6):485-90. doi: 10.1016/0883-2889(89)90131-7.
N-succinimidyl-3-(tri-n-butylstannyl)benzoate (m-BuATE), N-succinimidyl-3-(tri-methylstannyl)benzoate (m-MeATE) and N-succinimidyl-4-(tri-n-butylstannyl)benzoate (p-BuATE) were synthesized and radioiodinated using either N-chlorosuccinimide (NCS) or t-butylhydroperoxide (TBHP) as the oxidant. Radiohalogenation of m-MeATE proceeded more rapidly than m-BuATE. NCS was the more efficient oxidant at reaction times less than 15 min; use of both TBHP and NCS resulted in nearly quantitative yields after 15 min when m-MeATE was used. Using NCS, achieving optimal antibody coupling and specific binding required purification of the active ester by HPLC; in contrast, with TBHP, only Sep-Pak purification was needed.
合成了N-琥珀酰亚胺基-3-（三正丁基锡基）苯甲酸酯（间-丁基ATE）、N-琥珀酰亚胺基-3-（三甲基锡基）苯甲酸酯（间-甲基ATE）和N-琥珀酰亚胺基-4-（三正丁基锡基）苯甲酸酯（对-丁基ATE），并使用N-氯代琥珀酰亚胺（NCS）或叔丁基过氧化氢（TBHP）作为氧化剂进行放射性碘化。间-甲基ATE的放射性卤化比间-丁基ATE进行得更快。在反应时间少于15分钟时，NCS是更有效的氧化剂；当使用间-甲基ATE时，在15分钟后同时使用TBHP和NCS可获得几乎定量的产率。使用NCS时，通过高效液相色谱法（HPLC）纯化活性酯才能实现最佳的抗体偶联和特异性结合；相比之下，使用TBHP时，仅需Sep-Pak纯化。
