Process for making 5-lipoxygenase inhibitors having varied heterocyclic ring systems
US6344563B1 · kind B1 · utility
Inventors
Key dates
| Filing date | Jun 29, 2000 |
| Grant date | Feb 5, 2002 |
| Priority date | — |
| Expiry date | Jun 29, 2020 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D249/08
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
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 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: especially the substantially pure methanesulfonate salt thereof.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.