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Carrier‐free astatination of steroid hormones
Author(s) -
Pillai K. K. R.,
McLaughlin W. W.,
Lambrecht R. R.,
Bloomer W. W.
Publication year - 1987
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580240913
Subject(s) - chemistry , oxidizing agent , steroid , electrophile , hormone , combinatorial chemistry , molecule , steroid hormone , electrophilic substitution , organic chemistry , biochemistry , catalysis
The alpha emitting radiohalogen 211 At 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.