发明名称 |
PROCESS FOR MAKING 5-LIPOXYGENASE INHIBITORS HAVING VARIED HETEROCYCLIC RING SYSTEMS |
摘要 |
A process is described for preparing a compound of Formula (1.3.0): (see formula I) comprising: establishing a reaction mixture consisting of (see formula II) in an aprotic solvent; in the presence of NaOH or KOH; optionally in the presence of a phase transfer catalyst, especially a quaternary ammonium salt or a phosphonium salt; followed by heating said reaction mixture under a nitrogen atmosphere; 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); wherein the starting material of Formula (2.0.0) is prepared as follows: are reacted together in a solvent consisting of a straight or branched chain aliphatic alcohol; in the presence of a strong base consisting of NaOH or KOH; further in the presence of (see formula III) a transition metal catalyst comprising a palladium metal complex; and still further in the presence of an auxiliary ligand comprising a bidentate, chiral, axially dissymmetric aromatic compound of Formula (5.5.0) or (5.5.1): (see formula IV)
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申请公布号 |
CA2316748(A1) |
申请公布日期 |
2001.02.28 |
申请号 |
CA20002316748 |
申请日期 |
2000.08.29 |
申请人 |
PFIZER PRODUCTS INC. |
发明人 |
NORRIS, TIMOTHY;HNATOW, MEGAN ELIZABETH |
分类号 |
C07D309/04;A61K31/35;A61K31/351;A61K31/41;A61P9/00;A61P29/00;C07B61/00;C07C233/28;C07C233/64;C07C235/40;C07D;C07D233/64;C07D235/32;C07D309/02;C07D309/08;C07D309/32;C07D309/34;C07D403/12;C07D405/10;C07D405/12;C07D521/00;(IPC1-7):C07D405/12 |
主分类号 |
C07D309/04 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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