Iodinated estradiols, intermediate products and methods of production

摘要

A method of preparation of estradiol derivatives labeled by iodine, especially 123I, substitution at C-16 are synthesized according to the present invention. A triflate intermediate is prepared from which either 16-alpha-123I-17-beta-estradiol or 16-beta-123I-17-beta-estradiol are prepared by described methods. Both 16-alpha-123I- and 16-beta-123I-17-beta-estradiol made according to the methods described herein have a high relative specific acitvity. The methods are sufficiently rapid so that the relatively short half-life of 123I is readily accommodated without substantial radioactive decay of the label.