Carrier-free astatination of steroid hormones

The alpha emitting radiohalogen 211At has potential use as a radiotherapeutic agent when linked to biologically active molecules. The range of compounds which may be astatinated is limited by relative lack of knowledge of organoastatine syntheses. The production of astatovinyl steroids was carried out via electrophilic substitution of tri-n-butylstannylvinyl steroids with astatide in the presence of mild oxidizing agents. The astatinated steroids are synthesized rapidly and in carrier-free fashion yielding compounds of high radiochemical purity. (author)