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

Autor:	Lan Waterhouse, Itzela D. Correa, Shimoga R. Prakash, John J. Newman, Stephen Montgomery, Karl M. Cable, Guy N. Wells, Derek R. Sutherland, Lan Fellows
Rok vydání:	1995
Předmět:	Stereochemistry Aryl Organic Chemistry Methylene bridge Biochemistry Chemical synthesis Analytical Chemistry chemistry.chemical_compound chemistry Alosetron Drug Discovery Lactam medicine Radiology Nuclear Medicine and imaging Phosgene Paraformaldehyde Spectroscopy Phenylhydrazine medicine.drug
Zdroj:	Journal of Labelled Compounds and Radiopharmaceuticals. 36:993-1007
ISSN:	0362-4803
DOI:	10.1002/jlcr.2580361011
Popis:	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
Databáze:	OpenAIRE
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