发明授权
- 专利标题: Process for pyrimidinone compounds
- 专利标题(中): 嘧啶酮化合物的方法
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申请号: US207547申请日: 1998-12-08
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公开(公告)号: US6054582A公开(公告)日: 2000-04-25
- 发明人: Ping Zhou , Edward Curtis Taylor , Colin Michael Tice
- 申请人: Ping Zhou , Edward Curtis Taylor , Colin Michael Tice
- 申请人地址: PA Phila
- 专利权人: Rohm and Haas Company
- 当前专利权人: Rohm and Haas Company
- 当前专利权人地址: PA Phila
- 主分类号: B01J31/24
- IPC分类号: B01J31/24 ; C07B61/00 ; C07D239/36 ; C07D239/52 ; C07D239/60 ; C07D401/04 ; C07F7/08 ; C07D239/54
摘要:
This invention relates to a process for the preparation of pyrimidinone compounds of the formula ##STR1## wherein Ar is an optionally substituted aryl or heteroaromatic moiety,R.sup.3 is an optionally substituted alkyl, alkenyl or alkynyl,R.sup.5 is a hydrogen atom, halo, cyano or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy or alkylthio, andR.sup.6 is a hydrogen atom, cyano, or an optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, aralkyl or heteroaryl. The process comprises reaction of an amidine and a malonic acid derivative to give a hydroxypyrimidinone followed by conversion of the resulting hydroxypyrimidinone to a sulfonyloxypyrimidinone followed by reaction of the resulting sulfonyloxypyrimidinone with an organometallic reagent to give the desired pyrimidinone. The hydroxypyrimidinones, wherein R.sup.6 is hydroxy and sulfonyloxypyrimidinones wherein R.sup.6 is a substituted sulfonyloxy moiety, are themselves new and useful intermediates in the preparation of the desired pyrimidinones.
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