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A new route to 5,6‐diarylpyridazin‐3‐ones by metalation and cross‐coupling of pyridazines
Author(s) -
Trécourt F.,
Turck A.,
Plé N.,
Paris A.,
Quéguiner G.
Publication year - 1995
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570320364
Subject(s) - metalation , chemistry , regioselectivity , trimethylsilyl , combinatorial chemistry , stereochemistry , coupling (piping) , medicinal chemistry , organic chemistry , catalysis , mechanical engineering , engineering
Starting from 3,6‐dichloropyridazine, a new route is described to antihypertensive 5,6‐diarylpyridazin‐3‐ones. This pathway comprises the regioselective metalation followed by a substitution of the trimethylsilyl moeity. The introduction of iodine by another metalation allowed the cross coupling of arylboronic acids. The 6‐methoxy group was then cleaved to afford the pyridazinones.