Process for making 5-lipoxygenase inhibitors having varied...

Details Process for making 5-lipoxygenase inhibitors having varied... Process for making 5-lipoxygenase inhibitors having varied...

C - Chemistry, Metallurgy

07

D

C07D 405/12 (2006.01) C07D 309/08 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2317097

A novel process intermediate, tetrahydro-4-[3-(4-fluorophenyl)thio]phenyl-2H- pyran-4- carboxamide, of the formula: (see formula I) is described, as well as its use in a process of preparing 5-lipoxygenase inhibitors of the formula: (see formula II) which comprises establishing a reaction mixture consisting of: (see formula III) -and- an electron deficient monocyclic or benzo-fused bicyclic N-heterocycle containing two nitrogen atoms of the formula: (see formula IV to VII) 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.

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