m-[125I]iodoaniline: a useful reagent for radiolabeling biotin

Abstract

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.