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

作者: John F. Lambert , Timothy Norris , Megan E. Hnatow

DOI:

关键词: Salt (chemistry)SolventOrganic chemistryChlorideCatalysisSodium hydroxidePhase-transfer catalystChemistryPotassium hydroxidePhosphonium salt

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

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