发明授权
US6140515A Process of making 3-aryloxy, 4-aryl furan-2-ones useful as inhibitors of
COX-2
失效
制备3-芳氧基，4-芳基呋喃-2-酮可用作COX-2抑制剂的方法
- 专利标题： Process of making 3-aryloxy, 4-aryl furan-2-ones useful as inhibitors of COX-2
- 专利标题（中）： 制备3-芳氧基，4-芳基呋喃-2-酮可用作COX-2抑制剂的方法
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申请号： US153403申请日： 1998-09-15
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公开(公告)号： US6140515A公开(公告)日： 2000-10-31
- 发明人: Cheng Y. Chen , Lushi Tan , Robert D. Larsen
- 申请人： Cheng Y. Chen , Lushi Tan , Robert D. Larsen
- 申请人地址： NJ Rahway
- 专利权人： Merck & Co., Inc.
- 当前专利权人： Merck & Co., Inc.
- 当前专利权人地址： NJ Rahway
- 主分类号： C07D307/60
- IPC分类号： C07D307/60 ; C07D307/12 ; C07C315/00 ; C07D307/26 ; C07D401/12 ; C07D405/12
摘要：
Described is a process of preparing 3-aryl, 4-aryloxy furan-5-ones which are useful as inhibitors of cyclooxygenase-2 (COX-2). Such compounds are useful as anti-inflammatory agents. The process is directed to an asymmetric synthesis which involves: a trisubstituted styrene derivative preparation via Horner-Wadsworth-Emmons reaction and subsequent one pot trifluoromethylation of the allylic alcohol; preparation of the .alpha.-hydroxyl ketone using Sharpless asymmetric dihydroxylation and Swern oxidation; the esterification of the .alpha.-hydroxyl ketone with the phenoxy acetic acid; and the Dieckman condensation of the resulting ester.
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