Abstract
Some new estrogens based on the diethylstilbestrol structure have been prepared for use as diagnostic, radiopharmaceuticals. By the use of structure activity relationships the optimal position for the introduction of iodine was determined to be the α position. The new α-halostilbestrols were prepared as their dimethoxy, monomethoxy and dihydroxy forms. These forms were successfully labelled using82Br,125I,128I and131I. A rationale for the mode of incorporation of125I and131I was developed which also explained the stereochemistry of incorporation. This incorporation required the use of the cuprous ion as a catalyst. It was found that in the absence of such a catalyst the incorporation of radioiodide proceeded very slowly and without stereospecificity whereas in the presence of cuprous ion it was rapid and the configuration of the substrate was maintained.
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