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Synthesis of isotopically labelled pyridoindolone 5-HT3 receptor antagonists (1)

✍ Scribed by Shimoga R Prakash; Karl M Cable; Itzela D Correa; Lan Fellows; Stephen Montgomery; John J Newman; Lan Waterhouse; Guy N Wells; Derek R Sutherland

Publisher: John Wiley and Sons
Year: 1995
Tongue: French
Weight: 818 KB
Volume: 36
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580361011

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✦ Synopsis

Abstract

Syntheses of labelled versions of 5‐HT~3~ receptor antagonists, Alosetron and Lurosetron, are described. [^14^C]Alosetron was prepared by routes utilizing either Fischer indolisation of an amidohydrazine or palladium‐mediated cyclisation of an aryl enaminone as key steps. ^2^H and ^13^C versions of Alosetron were prepared from suitably labelled imidazoles. Lurosetron was labelled in either the methylene bridge carbon or carbonyl carbon, using ^14^C‐labelled paraformaldehyde or phosgene, respectively.

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