Process for preparing 5-lipoxygenase inhibitors with various heterocyclic systems

A process is described for preparing a compound of Formula (1.3.0): comprising: establishing a reaction mixture consisting of in an aprotic solvent; in the presence of NaOH or KOH; optionally in the presence of a phase transfer catalyst, especially a quaternary ammonium salt or a phosphonium salt; f...

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Bibliographic Details
Main Authors NORRIS TIMOTHY, HNATOW MEGAN ELIZABETH
Format Patent
LanguageCzech
English
Published 12.12.2001
Edition7
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
APPARATUS THEREFOR
CHEMISTRY
GENERAL METHODS OF ORGANIC CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:A process is described for preparing a compound of Formula (1.3.0): comprising: establishing a reaction mixture consisting of in an aprotic solvent; in the presence of NaOH or KOH; optionally in the presence of a phase transfer catalyst, especially a quaternary ammonium salt or a phosphonium salt; followed by heating said reaction mixture under a nitrogen atmosphere; in a preferred embodiment the aprotic solvent is DMSO, the strong base in solid form is NaOH in powder or pellet form, and the phase transfer catalyst is tetra-n-butylammonium chloride (TBAC); wherein the starting material of Formula (2.0.0) is prepared as follows: are reacted together in a solvent consisting of a straight or branched chain aliphatic alcohol; in the presence of a strong base consisting of NaOH or KOH; further in the presence of a transition metal catalyst comprising a palladium metal complex; and still further in the presence of an auxiliary ligand comprising a bidentate, chiral, axially dissymmetric aromatic compound of Formula (5.5.0) or (5.5.1):
Bibliography:Application Number: CZ20000003159