• Journal Article

Synthesis of [I-125]-3 beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester ([I-125]EINT)

Citation

Zhong, D., Blough, B., Kuhar, M. J., & Carroll, F. (2000). Synthesis of [I-125]-3 beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester ([I-125]EINT). Journal of Labelled Compounds and Radiopharmaceuticals, 43(2), 137-146.

Abstract

A WIN 35,065-2 analog, 3 beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester (EINT), has been radiolabeled with iodine-125 by radioiododestannylation of the trimethyltin derivative, N-tert-butoxycarbonyl-3 beta- (4-ethyl-3-trimethyltinphenyl)nortropane-2 beta- carboxylic acid methyl ester (2), using carrier-free sodium iodide-125. The radiolabeling consists of a one-pot, two-step method entailing radioiododestannylation followed by nitrogen deprotection. Purification by reversed-phase HPLC gives [I-125]EINT in 34.2% yield with high radiochemical purity (>99%) and high specific activity (1988 mCi/mu mol, 73.6 GBq/mu mol, based on the specific activity of the (NaI)-I-125 used)