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公开(公告)号：EP0912537B1
公开(公告)日：2004-05-12
申请号：EP97932424.1
申请日：1997-06-27
申请人： MERCK & CO., INC.
发明人： DESMOND, Richard , DOLLING, Ulf, H. , FREY, Lisa, F. , TILLYER, Richard, D. , TSCHAEN, David, M.
IPC分类号： C07D307/38
CPC分类号： C07D307/38
摘要： The invention encompasses a process for making compounds of Formula (I) useful in the treatment of inflammation and other cyclooxygenase-2 mediated diseases.
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公开(公告)号：EP0991651B1
公开(公告)日：2003-11-12
申请号：EP98931264.0
申请日：1998-06-12
申请人： MERCK & CO., INC.
发明人： WILLIAMS, John, M. , BRANDS, Karel, M., J. , SKERLJ, Renato, T. , DOLLING, Ulf, H. , JOBSON, Ronald, B.
IPC分类号： C07D477/20
CPC分类号： C07D477/20 , Y02P20/55
摘要： A stabilized carbapenem intermediate compound represented by formula (1) or a salt thereof is disclosed, wherein P represents a carboxyl protecting group and X represents a charge balancing group. In addition, a process for synthesizing a compound represented by formula (2) is disclosed wherein X+ is a charge balancing group, comprising: deprotecting a compound of formula (1) to produce a compound (2).
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公开(公告)号：EP0923556A1
公开(公告)日：1999-06-23
申请号：EP97936396.0
申请日：1997-08-05
申请人： MERCK & CO., INC.
CPC分类号： C07D401/04 , C07D263/06 , C07D405/06 , C07D413/04 , C07F7/1892
摘要： This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
摘要翻译： 本发明涉及合成内皮素拮抗剂的关键中间体和使用不对称共轭加成反应合成该关键中间体。
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公开(公告)号：EP0882026A1
公开(公告)日：1998-12-09
申请号：EP96944785.0
申请日：1996-12-12
CPC分类号： C07D239/22
摘要： The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a β-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu2O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.
摘要翻译： 本发明提供了一种通过结合β-酮酯或二酮，形成5-（烷基或烷氧基）羰基-6-烷基-4-（芳基或烷基）-3,4-2（1H） - 二氢嘧啶酮的方法， 醛和脲在硼试剂，金属盐（例如Cu 2 O）和催化剂（例如酸）存在下进行。 该反应通常在溶剂中在一个罐中进行，以比以前已知的方法更高的收率和更容易的后处理来提供二氢嘧啶酮。
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公开(公告)号：EP0923556B1
公开(公告)日：2003-10-08
申请号：EP97936396.7
申请日：1997-08-05
申请人： MERCK & CO., INC.
IPC分类号： C07D213/02 , C07D401/04 , C07D401/06 , A61K31/335 , A61K31/415 , A61K31/42 , A61K31/44
CPC分类号： C07D401/04 , C07D263/06 , C07D405/06 , C07D413/04 , C07F7/1892
摘要： This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
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公开(公告)号：EP1019411A1
公开(公告)日：2000-07-19
申请号：EP98933069.1
申请日：1998-07-02
申请人： MERCK & CO., INC.
发明人： BRANDS, Karel, M., J. , WILLIAMS, John, M. , DOLLING, Ulf, H. , JOBSON, Ronald, B. , DAVIES, Anthony, J. , COTTRELL, Ian, F. , CAMERON, Mark , ASHWOOD, Michael, S.
IPC分类号： C07D495/08 , C07D207/12
CPC分类号： C07D409/12 , C07D207/16 , C07D495/08 , C07F9/5721 , C07F9/5722
摘要： A process of synthesizing a compound of formula (1) is described. A compound of formula (2) is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula (4). Compound (4) is then reacted with a group II metal sulfide source in water to produce a compound of formula (1).
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公开(公告)号：EP0991651A1
公开(公告)日：2000-04-12
申请号：EP98931264.0
申请日：1998-06-12
申请人： MERCK & CO., INC.
发明人： WILLIAMS, John, M. , BRANDS, Karel, M., J. , SKERLJ, Renato, T. , DOLLING, Ulf, H. , JOBSON, Ronald, B.
IPC分类号： C07D477/20
CPC分类号： C07D477/20 , Y02P20/55
摘要： A stabilized carbapenem intermediate compound represented by formula (1) or a salt thereof is disclosed, wherein P represents a carboxyl protecting group and X represents a charge balancing group. In addition, a process for synthesizing a compound represented by formula (2) is disclosed wherein X+ is a charge balancing group, comprising: deprotecting a compound of formula (1) to produce a compound (2).
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公开(公告)号：EP0923557A1
公开(公告)日：1999-06-23
申请号：EP97937187.0
申请日：1997-08-08
发明人： DEVINE, Paul, N. , DOLLING, Ulf, H. , FREY, Lisa, F. , TILLYER, Richard, D. , TSCHAEN, David, M. , KATO, Yoshiaki
CPC分类号： C07D405/04
摘要： This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.
摘要翻译： 本发明涉及内皮素拮抗剂合成中的关键中间体，该关键中间体的合成以及使用该中间体在立体选择性脱氧反应中合成内皮素拮抗剂。
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公开(公告)号：EP1341784A2
公开(公告)日：2003-09-10
申请号：EP01992059.4
申请日：2001-12-04
发明人： DOLLING, Ulf, H. , ALABASTER, Ramon, J. , ASHWOOD, Michael, S. , COTTRELL, Ian, F. , COWDEN, Cameron, J. , DAVIES, Antony, J. , HANDS, David , WALLACE, Debra, J. , WILSON, Robert, D.
IPC分类号： C07D401/14 , A61K31/4427 , A61P7/02 , C07D213/55 , C07D213/30 , C07D213/38 , C07D241/18 , C07D213/83 , C07D241/16 , C07D401/12 , C07D213/61 , C07C235/74
CPC分类号： C07D213/30 , C07C235/74 , C07D213/38 , C07D213/55 , C07D213/61 , C07D213/83 , C07D213/84 , C07D241/16 , C07D241/18 , C07D401/12 , C07D401/14
摘要： The invention is a process for preparing 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide which comprises coupling with 2-aminomethyl-3-fluoropyridine dihydrochloric acid salt in the presence of a coupling reagent and a base to form 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide.
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公开(公告)号：EP0851850A1
公开(公告)日：1998-07-08
申请号：EP96930823.0
申请日：1996-09-11
申请人： MERCK & CO., INC.
CPC分类号： C07C319/20 , C07C45/004 , C07C45/45 , C07C259/06 , C07D317/54 , C07D333/22 , C07C323/22
摘要： A simple, high yielding synthesis of α-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-M-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.
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