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1.发明公开PROCESSES AND INTERMEDIATES FOR PREPARING A MACROCYCLIC PROTEASE INHIBITOR OF HCV 审中-公开PROCESS和中间产品用于生产HCV如下的大环蛋白酶抑制剂
公开(公告)号：EP2758386A1
公开(公告)日：2014-07-30
申请号：EP12762583.8
申请日：2012-09-21
IPC分类号： C07D311/06 , C07D417/04 , C07D453/04
CPC分类号： C07D453/02 , C07C235/82 , C07D311/06 , C07D417/04 , C07D453/04
摘要： Disclosed is a process for the preparation of a cinchonidine salt of formula (IV) via an aqueous solution of a racemic 4-hydroxy-1,2-cyclopentanedicarboxylic acid, which is subjected to cyclization without removing water, by the addition of a water- miscible organic solvent to the aqueous solution and, again without removing water, adding cinchonidine to the aqueous-organic solvent solution so as to obtain the cinchonidine salt of the lactone acid. The cinchonidine salt is allowd to crystallize so as to obtain the enantiomerically purified crystalline lactone acid cinchonidine salt (IV). The enantiomerically pure salt is an intermediate in the synthesis of HCV inhibitor compound of formula (I).
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2.发明公开IMPROVED PROCESS FOR PREPARING AN INTERMEDIATE OF THE MACROCYCLIC PROTEASE INHIBITOR TMC 435 有权改进的方法，产生中间从宏观循环蛋白酶抑制剂TMC 435
公开(公告)号：EP2771339A1
公开(公告)日：2014-09-03
申请号：EP12790677.4
申请日：2012-10-26
发明人： HORVATH, Andras , WUYTS, Stijn , DEPRÉ, Dominique Paul Michel , COUCK, Wouter Louis J , CUYPERS, Jozef Ludo Jan , HARUTYUNYAN, Syuzanna , BINOT, Gregory Fabien Sebastien
IPC分类号： C07D417/14
CPC分类号： C07D417/14 , C07D417/04
摘要： The present invention relates to an improved process for preparing (2R,3aR,10Z,11aS,2aR,14aR)-cyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxylic acid, 2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydro-2-[[7-methoxy-8-methyl-2-[4-10(1-methylethyl)-2-thiazolyl]-4-quinolinyl]oxy]-5-methyl-4,14-dioxo-, ethyl ester. This compound is an intermediate in the overall synthesis route of the macrocyclic compound TMC 435. TMC 435 is an inhibitor of NS3/4A protease which plays an important role in the replication of the hepatitis C virus.
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3.发明公开PROCESSES AND INTERMEDIATES FOR PREPARING A MACROCYCLIC PROTEASE INHIBITOR OF HCV 有权VERFAHREN UND ZWISCHENPRODUKTE ZUR HERSTELLUNG EINES MAKROCYCLISCHEN INHIBITORS VON HCV-PROTEASE
公开(公告)号：EP2382198A1
公开(公告)日：2011-11-02
申请号：EP09801447.5
申请日：2009-12-22
IPC分类号： C07D311/06 , C07D417/04 , C07D453/04
CPC分类号： C07C67/475 , C07C231/12 , C07C235/40 , C07C2601/08 , C07D307/33 , C07D417/04 , C07D453/04
摘要： The present invention relates to the cinchonidine salt useful in the preparation of intermediates for preparing a macrocyclic HCV inhibitor, as well as processes involving this salt.
摘要翻译： 本发明涉及可用于制备用于制备大环HCV抑制剂的中间体的辛可尼定盐以及涉及该盐的方法。
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4.发明公开PROCESSES AND INTERMEDIATES FOR PREPARING A MACROCYCLIC PROTEASE INHIBITOR OF HCV 审中-公开制备HCV的大环蛋白酶抑制剂的过程和中间体
公开(公告)号：EP3274324A1
公开(公告)日：2018-01-31
申请号：EP16715347.7
申请日：2016-03-25
发明人： DEPRÉ, Dominique Paul Michel , ORMEROD, Dominic John , HORVATH, Andras , MOODY, Thomas Shaw , BROSSAT, Maude , RIANT, Olivier , VRIAMONT, Nicolas , LEMAIRE, Sébastien François Emmanuel , HERMANT, Sébastien Nicolas J.
IPC分类号： C07C67/08 , C07C67/30 , C07C67/31 , C07C67/60 , C07D417/04 , C07D417/14 , C07C231/02 , C07C231/12
CPC分类号： C07C235/82 , C07B2200/07 , C07C67/31 , C07C69/757 , C07C231/02 , C07C231/12 , C07C233/60 , C07C233/61 , C07C2601/08 , C07D417/04 , C07D417/14 , C12P41/001
摘要： Disclosed is a process for the preparation of certain intermediates, e.g. those in the scheme below: which intermediates and processes are useful in the preparation of the macrocyclic HVC inhibitor Simeprevir.
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5.发明公开PROCESSES AND INTERMEDIATES FOR PREPARING A MACROCYCLIC PROTEASE INHIBITOR OF HCV 审中-公开制备HCV的大环蛋白酶抑制剂的过程和中间体
公开(公告)号：EP3239129A1
公开(公告)日：2017-11-01
申请号：EP17166514.4
申请日：2011-03-16
IPC分类号： C07C51/487
CPC分类号： C07D417/04 , C07B2200/07 , C07C51/02 , C07C51/412 , C07C51/43 , C07C61/06 , C07C67/03 , C07C67/31 , C07C69/757 , C07C201/12 , C07C205/57 , C07C215/20 , C07C215/30 , C07C231/12 , C07C235/40 , C07C235/82 , C07C255/57 , C07C317/44 , C07C2601/08 , C07D251/28 , C07D251/30 , C07D309/30 , C07D417/14 , C07D491/18 , C07D491/22 , C07C62/24
摘要： A process for preparing [(1 R ,2 R )-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising:
(a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or ( 1R,2S )-(-)-ephedrine, thus preparing the bis-brucine or bis-( 1R , 2S )-(-)-ephedrine salt of (V), and
(b) precipitating selectively the bis-brucine or bis-( 1R,2S )-( - )-ephedrine salt of (1 R ,2 R )-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis-( 1R,2S ) - (-)-ephedrine salt of [(1 S ,2 S )-4-oxo-1,2-cyclopentanedicarboxylic acid stays in solution;
(c) liberating the acid II by removal of brucine or ( 1R , 2S )-(-)-ephedrine from the precipitated salt obtained in step (b).摘要翻译： 通过拆分外消旋4-氧代-1,2-环戊烷二羧酸（V）制备[（1R，2R）-4-氧代-1,2-环戊烷二羧酸II的方法，所述方法包括：（a） （1R，2S） - （ - ） - 麻黄碱，由此制备双马钱果碱或双 - （1R，2S） - （ - ） - 麻黄碱盐 （V）和（b）选择性地沉淀（1R，2R）-4-氧代-1,2-环戊烷二羧酸II的双马钱果碱或双 - （1R，2S） - （ - ） - 麻黄碱盐， （1S，2S）-4-氧代-1,2-环戊烷二羧酸的双 - 马钱子碱或双 - （1R，2S） - （ - ） - 麻黄碱盐保留在溶液中; （c）通过从步骤（b）中获得的沉淀盐中除去马钱子碱或（1R，2S） - （ - ） - 麻黄碱而释放酸II。
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6.发明授权IMPROVED PROCESS FOR PREPARING AN INTERMEDIATE OF THE MACROCYCLIC PROTEASE INHIBITOR TMC 435 有权改进的制备大环内酯蛋白酶抑制剂中间体的方法TMC 435
公开(公告)号：EP2771339B1
公开(公告)日：2018-04-18
申请号：EP12790677.4
申请日：2012-10-26
发明人： HORVATH, Andras , WUYTS, Stijn , DEPRÉ, Dominique Paul Michel , COUCK, Wouter Louis J , CUYPERS, Jozef Ludo Jan , HARUTYUNYAN, Syuzanna , BINOT, Gregory Fabien Sebastien
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D417/14 , C07D417/04
摘要： The present invention relates to an improved process for preparing (2R,3aR,10Z,11aS,2aR,14aR)-cyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxylic acid, 2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydro-2-[[7-methoxy-8-methyl-2-[4-10(1-methylethyl)-2-thiazolyl]-4-quinolinyl]oxy]-5-methyl-4,14-dioxo-, ethyl ester. This compound is an intermediate in the overall synthesis route of the macrocyclic compound TMC 435. TMC 435 is an inhibitor of NS3/4A protease which plays an important role in the replication of the hepatitis C virus.
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7.发明授权PROCESSES AND INTERMEDIATES FOR PREPARING A MACROCYCLIC PROTEASE INHIBITOR OF HCV 有权过程和中间产品用于生产HCV蛋白酶的抑制剂的大环
公开(公告)号：EP2382198B1
公开(公告)日：2013-07-10
申请号：EP09801447.5
申请日：2009-12-22
IPC分类号： C07D311/06 , C07D417/04 , C07D453/04
CPC分类号： C07C67/475 , C07C231/12 , C07C235/40 , C07C2601/08 , C07D307/33 , C07D417/04 , C07D453/04
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