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Rosiglitazone maleate (BRL 49653‐C); the preparation of [ 14 C] and [ 3 H] isotopomers
Author(s) -
Kirefu Tabassum,
Landvatter Scott W,
Latter Alison J,
Lawrie Kenneth WM,
Morecombe Donald J,
Willcocks Kenneth
Publication year - 2001
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.458
Subject(s) - chemistry , rosiglitazone , yield (engineering) , isotopomers , tritium , catalysis , nuclear chemistry , medicinal chemistry , radiochemistry , organic chemistry , biochemistry , molecule , receptor , materials science , metallurgy , physics , nuclear physics
The glitazone insulin sensitisers are an important class of pharmaceuticals for the treatment of Type 2 diabetes. Syntheses of [ methyl ‐ 14 C] and [ 3 H]rosiglitazone maleate (BRL 49653‐C), marketed by SmithKline Beecham Pharmaceuticals as Avandia ® are described. [ Methyl ‐ 14 C]BRL 49653‐C was prepared in 5 steps in 12.6% overall radiochemical yield from K[ 14 C]CN. Catalytic reduction with tritium gas of a dibromo derivative gave [ 3 H]rosiglitazone with a specific activity of 58Ci/mmol. Copyright © 2001 John Wiley & Sons, Ltd.