专利检索 ap:("Merck & Co., Inc." OR "MERCK SHARP & DOHME LTD.") AND inv:"WALLACE, Debra, J." 第 1 页

1.

发明公开
PROCESS FOR MAKING A THROMBIN INHIBITOR 审中-公开
标题翻译：用于生产凝血酶抑制剂

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

申请人： Merck & Co., Inc. , MERCK SHARP & DOHME LTD.

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.

2.

发明公开
FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF 审中-公开
标题翻译：地层TETRA的取代的烯酰胺及其选择还原立体声

公开(公告)号：EP1765771A2

公开(公告)日：2007-03-28

申请号：EP05768999.4

申请日：2005-07-01

申请人： Merck & Co., Inc.

发明人： CAMPOS, Kevin, R. , KLAPARS, Artis , MCWILLIAMS, J. Christopher , SHULTZ, C. Scott , WALLACE, Debra, J. , CHEN, Alex, M. , FREY, Lisa, F. , PERESYPKIN, Andrey, V. , WANG, Yaling , WENSLOW, Robert, M. , CHEN, Cheng-Yi

IPC分类号： C07C233/00 , C07D211/72

CPC分类号： C07C231/18 , C07C253/14 , C07C309/73 , C07D213/64 , C07C255/56

摘要： The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).