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One‐pot synthesis of 3‐(1‐methylethyl)‐2‐(4‐methoxyphenyl)‐3H‐naphth‐[1,2‐d] [2‐ 14 C] imidazole
Author(s) -
Odasso G.,
Toja E.
Publication year - 1983
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.2580201008
Subject(s) - chemistry , imidazole , yield (engineering) , chemical synthesis , diamine , imidazoline receptor , analgesic , dehydrogenation , medicinal chemistry , pharmacokinetics , stereochemistry , organic chemistry , pharmacology , in vitro , biochemistry , medicine , materials science , metallurgy , catalysis
A one‐pot synthesis of 3‐(1‐methylethyl)‐2‐(4‐methoxyphenyl)‐3H‐naphth[1,2‐d] [2‐ 14 C]imidazole ( 1 ), a nonacidic antiinflammatory and analgesic agent, is described. The starting material, 2‐isopropylamino‐1‐nitronaphthalene ( 3 ) was hydrogenated, the resulting diamine ( 4 ) reacted with p‐[ carbonyl ‐ 14 C] anisaldehyde and the intermediate imidazoline ( 5 ) finally dehydrogenated to give ( 1 ) in a radiochemical yield of 63.4% with a radiochemical purity > 99%. The labelled compound has been used in pharmacokinetics and metabolism studies.