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3 H‐ and 14 C‐labelling of the aromatase inhibitor ZK 138723
Author(s) -
Gay J.,
Strehlke P.
Publication year - 1996
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/(sici)1099-1344(199604)38:4<349::aid-jlcr849>3.0.co;2-i
Subject(s) - chemistry , labelling , halogenation , aromatase , bromine , specific activity , derivative (finance) , tritium , thiophene , cyanide , radiochemistry , stereochemistry , organic chemistry , biochemistry , medicine , enzyme , physics , cancer , breast cancer , nuclear physics , financial economics , economics
Synthesis of the 3 H‐ and 14 C‐labelled aromatase inhibitor ZK138723 is described + . The 3 H‐label was obtained by dehalogenation of a 4,5‐diiodoimidazole derivative with tritium gas, yielding 30.8 mCi with a specific activity of 33.4 Ci/mmol. Bromine replacement in the thiophene α‐position by [ 14 C]cyanide afforded 25.9 mCi of the 14 C‐labelled material with a specific activity of 55.6 mCi/mmol.