Synthesis of carbon-14 labelled indolic 5HT1 receptor agonists

Syntheses of carbon‐14 labelled versions of indolic 5HT1 agonists sumatriptan (GR43175) (1a), GR40370 (2a) and naratriptan (GR85548) (3a) are described. Introduction of the label via cyanation of ketoformanilides, formed by oxidative cleavage of an indole ring, ensured incorporation of carbon‐14 at...

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Bibliographic Details
Published inJournal of labelled compounds & radiopharmaceuticals Vol. 38; no. 11; pp. 1021 - 1030
Main Authors Waterhouse, Ian, Cable, Karl M, Fellows, Ian, Wipperman, Mark D, Sutherland, Derek R
Format Journal Article
LanguageEnglish
Published Chichester John Wiley & Sons, Ltd 01.11.1996
Wiley
Subjects
5HT1 receptor agonist
carbon-14
Chemistry
Exact sciences and technology
Heterocyclic compounds
Heterocyclic compounds with only one n hetero atom and condensed derivatives
indole
Organic chemistry
Preparations and properties
5-HT1 receptor
Agonist
Sulfonamide
Radiolabelling
Nitrogen heterocycle
Tertiary amine
Carbon Isotopes
Bicyclic compound
Aromatic compound
Indole derivatives
Chemical synthesis
Carbon 14
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Summary:Syntheses of carbon‐14 labelled versions of indolic 5HT1 agonists sumatriptan (GR43175) (1a), GR40370 (2a) and naratriptan (GR85548) (3a) are described. Introduction of the label via cyanation of ketoformanilides, formed by oxidative cleavage of an indole ring, ensured incorporation of carbon‐14 at the metabolically stable C‐2 position of the indole.
Bibliography:istex:BE235C6D7B08EF16D948E9DE952EC0C7CD5BCFC4
ark:/67375/WNG-TP40Q244-3
ArticleID:JLCR921
ISSN:0362-4803
1099-1344
DOI:10.1002/(SICI)1099-1344(199611)38:11<1021::AID-JLCR921>3.0.CO;2-O