HALOGEN LABELED COMPOUNDS INCLUDING ESTRADIOL DERIVATIVES, SYNTHETIC INTERMEDIATES, SYNTHESES THEREOF AND USES THEREOF

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 16alpha-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 activity. The methods are sufficiently rapid so that the relatively short half-life of 123I is readily accommodated without substantial radioactive decay of the label. A process for detecting a presence of steroid receptors in tissue especially tissue having estrogen receptors, includes the step of treating the tissue by injection, surface application or the like, with a labeled steroid. The labeled steroid may include a moiety which is readily imageable on a gamma radiation detector, on x-ray film, on a fluoroscope, through NMR devices or the like. An especially suitable labeled steroid has been found to be 16123I-17-beta-estradiol having a specific activity of greater than 2,000 curies per millimole and preferably at least 5,000 curies per millimole.