Khawli L A, Kassis A I
Department of Radiology (Nuclear Medicine), Harvard Medical School, Shields Warren Radiation Laboratory, Boston, MA 02115.
Int J Rad Appl Instrum B. 1992 Apr;19(3):297-301. doi: 10.1016/0883-2897(92)90114-e.
Biotinyl-m-[125I]iodoanilide (BIA) was synthesized by coupling biotin to m-[125I]iodoaniline via a mixed anhydride reaction. m-[125I]Iodoaniline was produced from the tin precursor, which was prepared using a palladium catalyzed reaction of hexabutylditin with m-bromoaniline. The radioiodinated BIA derivative is characterized by a stable amide and/or intact ureido group on the biotin molecule; it may thus be a useful carrier for targeting radionuclides to avidin-conjugated antibodies previously localized on tumors.
生物素化间-[¹²⁵I]碘苯胺（BIA）通过混合酸酐反应将生物素与间-[¹²⁵I]碘苯胺偶联合成。间-[¹²⁵I]碘苯胺由锡前体产生，该锡前体通过钯催化的六丁基二锡与间溴苯胺的反应制备。放射性碘化的BIA衍生物的特征在于生物素分子上有稳定的酰胺和/或完整的脲基；因此它可能是一种有用的载体，用于将放射性核素靶向先前定位在肿瘤上的抗生物素蛋白偶联抗体。
