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Syntheses of isotopically labelled angiotensin II receptor antagonist GR138950X

✍ Scribed by Richard M. Carr; Karl M. Cable; John J. Newman; Derek R. Sutherland

Publisher
John Wiley and Sons
Year
1996
Tongue
French
Weight
798 KB
Volume
38
Category
Article
ISSN
0022-2135

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✦ Synopsis

Syntheses of [I 3C

] and [14C]-labelled versions of angiotensin I1 receptor antagonist GR138950X, labelled in the imidazole carboxamide residue, are described. These involved preparation of an iodoimidazole substrate by a novel iododecarboxylation procedure, followed by cyanation with a mixture of carbon-labelled potassium cyanide and copper (I) iodide in DMF at high temperature. The preparation of a mass-labelled (M+5) version of GR138950X is also described. This involved the synthesis of an [13C3,15N2]-labelled imidazole from a 1,2,3-tricarbonyl compound, [13C3]propionaldehyde and [I 5N]ammonia. The labelled imidazole was further elaborated into multiply-labelled GRI 38950X.

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