SYNTHESIS OF ISOTOPICALLY LABELED PYRIDOINDOLONE 5-HT3 RECEPTOR ANTAGONISTS

Authors
PRAKASH SR CABLE KM CORREA ID FELLOWS I MONTGOMERY S NEWMAN JJ WATERHOUSE I WELLS GN SUTHERLAND DR
Citation
Sr. Prakash et al., SYNTHESIS OF ISOTOPICALLY LABELED PYRIDOINDOLONE 5-HT3 RECEPTOR ANTAGONISTS, Journal of labelled compounds & radiopharmaceuticals, 36(10), 1995, pp. 993-1007
Citations number
11
Categorie Soggetti
Chemistry Analytical","Pharmacology & Pharmacy","Biochemical Research Methods
Journal title
Journal of labelled compounds & radiopharmaceuticals → ACNP
ISSN journal
03624803
Volume
36
Issue
10
Year of publication
1995
Pages
993 - 1007
Database
ISI
SICI code
0362-4803(1995)36:10<993:SOILP5>2.0.ZU;2-A
Abstract
Syntheses of labelled versions of 5-HT3 receptor antagonists, Alosetro n and Lurosetron, are described, [C-14]Alosetron was prepared by route s utilizing either Fischer indolisation of an amidohydrazine or pallad ium-mediated cyclisation of an aryl enaminone as key steps. H-2 and C- 13 versions of Alosetron were prepared from suitably labelled imidazol es. Lurosetron was labelled in either the methylene bridge carbon or c arbonyl carbon, using C-14-labelled paraformaldehyde or phosgene, resp ectively.