Process for making 5-lipoxygenase inhibitors having varied heterocyclic ring systems

A novel process intermediate, tetrahydro-4- 3-(4-fluorophenyl)thio­phenyl-2H-pyran-4-carboxamide, of the formula: is described, as well as its use in a process of preparing 5-lipoxygenase inhibitors of the formula: which comprises establishing a reaction mixture consisting of: - and - an electron de...

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Bibliographic Details
Main Authors TIMOTHY NORRIS, MEGAN ELIZABETH HNATOW, JOHN FRANCIS LAMBERT
Format Patent
LanguageEnglish
Published 28.02.2002
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 novel process intermediate, tetrahydro-4- 3-(4-fluorophenyl)thio­phenyl-2H-pyran-4-carboxamide, of the formula: is described, as well as its use in a process of preparing 5-lipoxygenase inhibitors of the formula: which comprises establishing a reaction mixture consisting of: - and - an electron deficient monocyclic or benzo-fused bicyclic N-heterocycle containing two nitrogen atoms of the formula: in an aprotic solvent; in the presence of a carbonate of the formula: (M)2-CO3, where M is an alkali metal, Group 1/Ia element, selected from the group consisting of lithium, Li; sodium,Na; potassium, K; rubidium, Rb; and cesium, Cs; followed by heating of said reaction mixture under a nitrogen atmosphere; whereby there is produced the desired compound of the above-recited formula.
Bibliography:Application Number: ZA20000004435