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

摘要

A method of preparation of estradiol derivativeslabeled by iodine, especially 123I, substitution at C-16are synthesized according to the present invention. Atriflate intermediate is prepared from which either 16-alpha-123I-17-beta-estradiol or 16-beta-123I-17-beta-estradiol are prepared by described methods. Both16-alpha-123I- and 16-beta-123I-17-beta-estradiolmade according to the methods described herein have a highrelative specific activity. The methods are sufficientlyrapid so that the relatively short half-life of 123I isreadily accommodated without substantial radioactive decayof the label. A process for detecting a presence of steroidreceptors in tissue especially tissue having estrogenreceptors, includes the step of treating the tissue byinjection, surface application or the like, with a labeledsteroid. The labeled steroid may include a moiety which isreadily imageable on a gamma radiation detector, on x-rayfilm, on a fluoroscope, through NMR devices or the like. Anespecially suitable labeled steroid has been found to be 16-123I-17-beta-estradiol having a specific activity ofgreater than 2,000 curies per millimole and preferably atleast 5,000 curies per millimole.