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 235/06 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2317001

A process is described for preparing a compound of Formula (1.3.0): where (see formula I to III) comprising: establishing a reaction mixture consisting of (see formula IV and V) in an aprotic solvent; in the presence of a strong base in solid form selected from the group consisting of sodium hydroxide, NaOH; and potassium hydroxide, KOH; - and optionally - in the presence of a catalytic amount of cesium carbonate, Cs2CO3, or of a phase transfer catalyst, especially a quaternary ammonium salt or a phosphonium salt - followed by - heating said reaction mixture under a nitrogen atmosphere; whereby there is produced a compound of Formula (1.3.0); and 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), which is used to prepare a preferred compound, useful as a 5-lipoxygenase inhibitor, of the formula: (see formula VI) and especially the substantially pure methanesulfonate salt thereof.

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