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Synthesis of carbon-14 labelled indolic 5HT1 receptor agonists

✍ Scribed by Ian Waterhouse; Karl M Cable; Ian Fellows; Mark D Wipperman; Derek R Sutherland

Publisher: John Wiley and Sons
Year: 1996
Tongue: French
Weight: 523 KB
Volume: 38
Category: Article
ISSN: 0022-2135
DOI: 10.1002/(sici)1099-1344(199611)38:11<1021::aid-jlcr921>3.0.co;2-o

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✦ Synopsis

Syntheses of carbon-14 labelled versions of indolic 5HT1 agonists sumatriptan (GR43175) ( 1 ) , GR40370 (2a) and naratriptan (GR85548) (3a) are described.

Introduction of the label via cyanation of ketoforrnanilides, formed by oxidative cleavage of an indole ring, ensured incorporation of carbon-14 at the metabolically stable C-2 position of the indole.

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