Rosiglitazone maleate (BRL 49653-C); the preparation of [14C] and [3H] isotopomers

The glitazone insulin sensitisers are an important class of pharmaceuticals for the treatment of Type 2 diabetes. Syntheses of [methyl‐14C] and [3H]rosiglitazone maleate (BRL 49653‐C), marketed by SmithKline Beecham Pharmaceuticals as Avandia® are described. [Methyl‐14C]BRL 49653‐C was prepared in 5...

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Veröffentlicht in:	Journal of labelled compounds & radiopharmaceuticals 2001-04, Vol.44 (5), p.329-335
Hauptverfasser:	Kirefu, Tabassum, Landvatter, Scott W, Latter, Alison J, Lawrie, Kenneth WM, Morecombe, Donald J, Willcocks, Kenneth
Format:	Artikel
Sprache:	eng
Schlagworte:	Avandia Biological and medical sciences BRL 49653 carbon-14 Chemistry Exact sciences and technology General and cellular metabolism. Vitamins glitazone Heterocyclic compounds Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms Medical sciences Organic chemistry Pharmacology. Drug treatments Preparations and properties rosiglitazone tritium type 2 diabetes
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Beschreibung
Zusammenfassung:	The glitazone insulin sensitisers are an important class of pharmaceuticals for the treatment of Type 2 diabetes. Syntheses of [methyl‐14C] and [3H]rosiglitazone maleate (BRL 49653‐C), marketed by SmithKline Beecham Pharmaceuticals as Avandia® are described. [Methyl‐14C]BRL 49653‐C was prepared in 5 steps in 12.6% overall radiochemical yield from K[14C]CN. Catalytic reduction with tritium gas of a dibromo derivative gave [3H]rosiglitazone with a specific activity of 58Ci/mmol. Copyright © 2001 John Wiley & Sons, Ltd.
ISSN:	0362-4803 1099-1344
DOI:	10.1002/jlcr.458