Abstract
Iodination of the A-ring of estradiol was performed by treating estradiol with iodine (I2) in the presence of mercuric acetate. Although this procedure has generally been considered as a selective preparation method for 2-iodoestradiol, we found that two major products were obtained from the reaction. These compounds were separated clearly by silica gel medium-pressure liquid chromatography, using benzene-acetone (5:1, v/v) as a mobile phase. The two compounds were identified as 2-iodoestradiol (36.8% yield) and 4-iodoestradiol (21.5% yield) based on physicochemical data, and in particular on 1H-NMR spectra.
