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Synthesis of isotopically labelled pyridoindolone 5‐HT 3 receptor antagonists (1)
Author(s) -
Prakash Shimoga R,
Cable Karl M,
Correa Itzela D,
Fellows Lan,
Montgomery Stephen,
Newman John J,
Waterhouse Lan,
Wells Guy N,
Sutherland Derek R
Publication year - 1995
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580361011
Subject(s) - chemistry , paraformaldehyde , phosgene , combinatorial chemistry , stereochemistry , organic chemistry
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.