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Reduction of iminium ethers with sodium boro[ 3 H] hydride. Preparation of tritium labelled clomiphene and nitromiphene (CI 628)
Author(s) -
Ruenitz Peter C.,
Bagley Jerome R.
Publication year - 1984
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.2580210909
Subject(s) - chemistry , iminium , yield (engineering) , radiochemistry , reagent , specific activity , tritium , hydride , sodium hydride , sodium , boro , in vivo , nuclear chemistry , medicinal chemistry , organic chemistry , enzyme , boron , hydrogen , ion , materials science , physics , microbiology and biotechnology , nuclear physics , metallurgy , biology
The preparation of [ 3 H]‐clomiphene and [ 3 H]‐nitromiphene from amido precursors in a two‐step reaction sequence utilizing NaB H 4 is described. The radiochemical yield and specific activity of the former are 34% and 16 mCi/mmol and those of the latter were 42% and 20 mCi/mmol, respectively. The method described is of micromolar scale designed for maintaining cost economy in the purchase of expensive radiolabelled reagents while yielding final products of sufficient radioactivity for in vitro and in vivo metabolism studies.