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The preparation of carbon‐14 and tritium labelled 1‐[4‐(2‐dimethylaminoethoxy) phenyl]‐1, 2‐diphenyl‐1‐butene [ICI 46,474, tamoxifen (nolvadex )] and the separation of cis‐trans isomers 2. The synthesis of tritium labelled tamoxifen (nolvadex )
Author(s) -
Burns J.,
Richardson O. N.
Publication year - 1982
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.2580190406
Subject(s) - chemistry , tritium , tamoxifen , tritiated water , specific activity , carbon 14 , bromobenzene , catalysis , radiochemistry , organic chemistry , medicine , physics , cancer , quantum mechanics , breast cancer , nuclear physics , enzyme
The preparation of tritiated tamoxifen generally labelled, and also specifically labelled in two separate positions is described. The generally tritiated material was prepared by an acid catalysed exchange reaction which produced labelled material of low molar specific activity [4.7 mCi/mmol]. Both specifically tritiated products were derived from tritium labelled intermediates which were used in synthetic procedures to produce tritiated tamoxifen. [G‐ 3 H]Bromobenzene was used to incorporate the label in the 1‐phenyl ring, and tamoxifen with a specific activity of 401 mCi/mmol was obtained. The reductive tritiation of a 3, 5‐dibromo precursor and subsequent synthesis gave tamoxifen with a specific activity of 19.5 Curies/ mmol.