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1.发明申请FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF 审中-公开四唑替代方法的形成及其选择性减少公开(公告)号：US20100041893A1
公开(公告)日：2010-02-18
申请号：US12603901
申请日：2009-10-22
申请人： KEVIN R. CAMPOS , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： KEVIN R. CAMPOS , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D211/72 , C07C233/00
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).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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2.发明授权公开(公告)号：US07629470B2
公开(公告)日：2009-12-08
申请号：US11629005
申请日：2005-07-01
申请人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D213/63
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).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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3.发明申请公开(公告)号：US20090018340A1
公开(公告)日：2009-01-15
申请号：US11629005
申请日：2005-07-01
申请人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D213/64 , C07C255/50
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).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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公开(公告)号：US20170275327A1
公开(公告)日：2017-09-28
申请号：US15503776
申请日：2015-08-14
申请人： John Simon EDWARDS , Peter Richard MULLENS , Edward CLEATOR , Bryon L. SIMMONS , Courtney K. MAGUIRE , Jeremy Peter SCOTT , Nobuyoshi YASUDA , Yong ZHONG , Lisa F. FREY , Peter G. DORMER , Andrew BRUNSKILL , Artis KLAPARS , Eric ASHLEY , Pu QIAN , Yi ZHANG , Baoqiang WAN , MERCK SHARP & DOHME CORP. , MERCK SHARP & DOHME LIMITED
发明人： John Edwards , Peter Richard Mullens , Ed Cleator , Bryon L. Simmons , Courtney K. Maguire , Jeremy Peter Scott , Nobuyoshi Yasuda , Yong-Li Zhong , Lisa F. Frey , Peter G. Dormer , Andrew Brunskill , Artis Klapars , Puneet Qian , Yi Zhang , Baoqiang Wan
CPC分类号： C07H19/10 , C07F9/242 , C07F9/2458 , C07F9/2487 , C07F9/58 , C07F9/65586 , C07H19/06
摘要： The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.
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公开(公告)号：US10526363B2
公开(公告)日：2020-01-07
申请号：US15503776
申请日：2015-08-14
申请人： Merck Sharp & Dohme Corp. , Merck Sharp & Dohme Limited , John Simon Edwards , Peter Richard Mullens , Edward Cleator , Bryon L. Simmons , Courtney K. Maguire , Jeremy Peter Scott , Nobuyoshi Yasuda , Yong-Li Zhong , Lisa F. Frey , Peter G. Dormer , Andrew Brunskill , Artis Klapars , Pu Qian , Yi Zhang , Baoqiang Wan , Eric Ashley
发明人： John Simon Edwards , Peter Richard Mullens , Edward Cleator , Bryon L. Simmons , Courtney K. Maguire , Jeremy Peter Scott , Nobuyoshi Yasuda , Yong-Li Zhong , Lisa F. Frey , Peter G. Dormer , Andrew Brunskill , Artis Klapars , Pu Qian , Yi Zhang , Baoqiang Wan , Eric Ashley
IPC分类号： C07H19/10 , C07F9/58 , C07H19/06 , C07F9/24 , C07F9/6558
摘要： The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.
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公开(公告)号：US5922864A
公开(公告)日：1999-07-13
申请号：US18204
申请日：1998-02-03
IPC分类号： C07C271/28 , C07D265/18
CPC分类号： C07D265/18 , C07C271/28 , C07C2101/02
摘要： An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl- 1,4-dihydro-2H-3, 1-benzoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.
摘要翻译： 制备（ - ） - 6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1-苯并恶嗪-2-酮化合物的有效方法，也称为DMP-266 ，使用氨基醇中间体与氯甲酸烷基酯或芳基酯和碱的环化反应来实现逆转录酶抑制剂。
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7.发明授权
公开(公告)号：US5840924A
公开(公告)日：1998-11-24
申请号：US876894
申请日：1997-06-16
IPC分类号： C07D307/58 , 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.
摘要翻译： 本发明包括制备式I化合物可用于治疗炎症和其它环加氧酶-2介导的疾病的方法。
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8.发明授权
公开(公告)号：US6114569A
公开(公告)日：2000-09-05
申请号：US224923
申请日：1999-01-04
IPC分类号： C07C271/28 , C07D265/18
CPC分类号： C07D265/18 , C07C271/28 , C07C2101/02
摘要： An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.
摘要翻译： 制备（ - ） - 6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1-苯并恶嗪-2-酮的化合物的有效方法，也称为DMP-266 ，使用氨基醇中间体与氯甲酸烷基酯或芳基酯和碱的环化反应来实现逆转录酶抑制剂。
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公开(公告)号：US5786515A
公开(公告)日：1998-07-28
申请号：US706041
申请日：1996-08-30
IPC分类号： C07C45/00 , C07C45/45 , C07C319/20 , C07C323/22 , C07D317/54 , C07D333/22 , C07C45/62
CPC分类号： C07D333/22 , C07C319/20 , C07C45/004 , C07C45/45 , C07D317/54
摘要： A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.
摘要翻译： 描述了一种简单的，高产率的α-氯代酮合成，涉及用N-甲氧基-N-甲基氯乙酰胺对格利雅德和有机锂试剂进行酰化。 通过再循环N，O-二甲基羟胺，进一步提高了该方法的效率。
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公开(公告)号：US06268510B1
公开(公告)日：2001-07-31
申请号：US09610780
申请日：2000-07-06
申请人： Lisa F. Frey , Edward J. J. Grabowski , Stephane G. Ouellet , Robert A. Reamer , Richard D. Tillyer
发明人： Lisa F. Frey , Edward J. J. Grabowski , Stephane G. Ouellet , Robert A. Reamer , Richard D. Tillyer
IPC分类号： C07D48712
CPC分类号： C07D487/04 , C07D221/16 , Y02P20/55
摘要： A rearrangement process for the preparation of a 6,5,5-tricyclic, a 6,6,5-tricyclic and 6,5,5,7-tetracyclic ring system is disclosed.
摘要翻译： 公开了制备6,5,5-三环，6,6,5-三环和6,5,5,7-四环体系的重排方法。
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