发明名称 Process for making 5-lipoxygenase inhibitors having varied heterocyclic ring systems
摘要 process is described for preparing a compound of Formula (1.3.0):comprising: establishing a reaction mixture consisting ofin 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.
申请公布号 US6344563(B1) 申请公布日期 2002.02.05
申请号 US20000606609 申请日期 2000.06.29
申请人 NORRIS TIMOTHY;HNATOW MEGAN E.;LAMBERT JOHN F. 发明人 NORRIS TIMOTHY;HNATOW MEGAN E.;LAMBERT JOHN F.
分类号 C07D405/12;A61K31/4155;A61K31/416;A61K31/4178;A61K31/4184;A61P1/00;A61P11/00;A61P19/06;A61P29/00;A61P37/00;A61P43/00;C07B61/00;C07D233/56;C07D235/06;C07D405/14;C07D521/00;(IPC1-7):C07D233/56 主分类号 C07D405/12
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