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

Kirefu Tabassum | Zendy; Landvatter Scott W | Zendy; Latter Alison J | Zendy; Lawrie Kenneth WM | Zendy; Morecombe Donald J | Zendy; Willcocks Kenneth | Zendy

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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.

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