发明授权
US6057445A Purine compounds having PDE IV inhibitory activity and methods of
synthesis
失效
具有PDE IV抑制活性的嘌呤化合物和合成方法
- 专利标题： Purine compounds having PDE IV inhibitory activity and methods of synthesis
- 专利标题（中）： 具有PDE IV抑制活性的嘌呤化合物和合成方法
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申请号： US209664申请日： 1998-12-10
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公开(公告)号： US6057445A公开(公告)日： 2000-05-02
- 发明人: David J. Cavalla , Mark Chasin , Peter Hofer
- 申请人： David J. Cavalla , Mark Chasin , Peter Hofer
- 申请人地址： LUX
- 专利权人： Euro-Celtique S.A.
- 当前专利权人： Euro-Celtique S.A.
- 当前专利权人地址： LUX
- 主分类号： A61K31/52
- IPC分类号： A61K31/52 ; A61K31/53 ; A61P11/00 ; A61P11/06 ; A61P25/24 ; A61P25/28 ; A61P27/16 ; A61P29/00 ; A61P29/02 ; A61P31/18 ; A61P37/04 ; A61P37/08 ; A61P43/00 ; C07D471/04 ; C07D473/30 ; C07D473/34 ; C07D487/04 ; C07D213/75 ; C07D239/46
摘要：
The present invention comprises methods of synthesizing compounds having the formula I: ##STR1## wherein: Y.sub.1, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.8 are as described herein, which comprises the steps of(a) reacting a compound of the formula III ##STR2## with a base to cause cyclization to compound IV ##STR3## (b) transforming said hydroxy group of said compound IV to an amine by successive halogenation by a halogenating agent and displacement of the resultant halogen with an amide to form compound V ##STR4## (c) reacting said compound V with an effective amount of compound VI ##STR5## to form the compound of formula 1.
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