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1. 发明授权

US5648511A Method for making intermediates useful in the synthesis of retroviral protease inhibitors 失效
标题翻译：制备可用于合成逆转录病毒蛋白酶抑制剂的中间体的方法
公开(公告)号：US5648511A
公开(公告)日：1997-07-15
申请号：US452187
申请日：1995-05-25
申请人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman , John J. Freskos , Gary A. DeCrescenzo , Deborah E. Bertenshaw , Robert M. Heintz , Suhong Zhang , Chin Liu , Scott A. Laneman
发明人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman , John J. Freskos , Gary A. DeCrescenzo , Deborah E. Bertenshaw , Robert M. Heintz , Suhong Zhang , Chin Liu , Scott A. Laneman
IPC分类号： A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C07C213/00 , C07C213/02 , C07C213/08 , C07C215/28 , C07C269/04 , C07C269/06 , C07C271/16 , C07F7/18 , C07K5/078 , C07D253/00
CPC分类号： C07C269/06 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07C213/00 , C07C213/02 , C07C213/08 , C07C269/04 , C07F7/188 , C07K5/06139 , A61K38/00 , C07B2200/07
摘要： A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.
摘要翻译：对于易于大规模制备基于羟基脲的手性HIV蛋白酶抑制剂的中间体描述了合成。该方法包括由手性α氨基醛形成非对映选择性环氧化物或羟腈。

2. 发明授权

US5610296A Process for the preparation of amidino phenyl pyrrolidine beta-alanine urea analogs 失效
标题翻译：制备脒基苯基吡咯烷β-丙氨酸脲类似物的方法
公开(公告)号：US5610296A
公开(公告)日：1997-03-11
申请号：US349333
申请日：1994-12-05
申请人： Norman A. Abood , Daniel L. Flynn , Scott A. Laneman , Roger Nosal , Lori A. Schretzman
发明人： Norman A. Abood , Daniel L. Flynn , Scott A. Laneman , Roger Nosal , Lori A. Schretzman
IPC分类号： A61K31/40 , A61K31/4015 , A61P7/02 , C07C323/60 , C07D207/26 , C07D207/273 , C07D207/12
CPC分类号： C07D207/273
摘要： The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
摘要翻译：本发明涉及通过在碱存在下在合适的非质子溶剂中通过用三甲基锍卤化物或三甲基氧化锍卤化物处理甲硫氨酸类似物，从式IMA图谱的甲硫氨酸类似物制备式“的内酰胺的方法。本发明进一步涉及使用这种甲硫氨酸和内酰胺化合物作为中间体制备脒基苯基吡咯烷基β-丙氨酸脲类似物，β-丙氨酸脲类似物可用作抗血栓形成剂。

3. 发明授权

US5484946A Process for the preparation of amidino phenyl pyrrolidine .beta.-alanine urea analogs 失效
公开(公告)号：US5484946A
公开(公告)日：1996-01-16
申请号：US463657
申请日：1995-06-05
申请人： Norman A. Abood , Daniel L. Flynn , Scott A. Laneman , Roger Nosal , Lori A. Schretzman
发明人： Norman A. Abood , Daniel L. Flynn , Scott A. Laneman , Roger Nosal , Lori A. Schretzman
IPC分类号： A61K31/40 , A61K31/4015 , A61P7/02 , C07C323/60 , C07D207/26 , C07D207/273
CPC分类号： C07D207/273
摘要： The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.

4. 发明授权

US5874628A Method for preparation of tertiary phosphines via nickel-catalyzed cross coupling 失效
标题翻译：通过镍催化交叉偶联制备叔膦的方法
公开(公告)号：US5874628A
公开(公告)日：1999-02-23
申请号：US824309
申请日：1997-03-26
申请人： Scott A. Laneman , David J. Ager , Amihia Eisenstadt
发明人： Scott A. Laneman , David J. Ager , Amihia Eisenstadt
IPC分类号： B01J31/26 , C07B61/00 , C07F9/50
CPC分类号： C07F9/5068
摘要： The invention is an improved method for the preparation of tertiary phosphines by way of cross-coupling of aryl, alkenyl, cycloalkenyl or aralkyl halides or aryl, alkenyl, cycloalkenyl or aralkyl sulfonate esters with chlorophosphines in the presence of a catalyst and a reductant. The general reaction scheme is shown below: ##STR1## wherein R.sup.1 is aryl, alkenyl, cycloalkenyl or aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl, or CONR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; R.sup.2 and R.sup.3 are independently aryl, alkyl, aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl or CoNR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; and n is 2 where R.sup.1 is a difunctional moiety and 1 for any other R.sup.1 ; and X is Cl, Br, I, or OSO.sub.2 Y; wherein Y is alkyl, trihalomethyl, phenyl, halophenyl, or alkylphenyl.
摘要翻译：本发明是通过芳基，链烯基，环烯基或芳烷基卤化物或芳基，烯基，环烯基或芳烷基磺酸酯与氯膦在催化剂和还原剂存在下交叉偶联来制备叔膦的改进方法。一般反应方案如下所示：其中R 1为芳基，烯基，环烯基或芳烷基，其中任何一个可被一个或多个下列基团取代：烷基，芳基，芳烷基，烷氧基，烷酰基，氯，氟，烷氧基羰基，氰基，三氟甲基，环烷基或CONR 4 R 5，其中R 4和R 5独立地是氢，烷基，芳基或芳烷基; R 2和R 3独立地为芳基，烷基，芳烷基，其中任一个可以被一个或多个下列基团取代：烷基，芳基，芳烷基，烷氧基，烷酰基，氯，氟，烷氧基羰基，氰基，三氟甲基，环烷基或CoNR 4 R 5，其中R 4 和R 5独立地是氢，烷基，芳基或芳烷基; 并且n为2，其中R 1为双官能部分，1为任何其它R 1; X为Cl，Br，I或OSO 2 Y; 其中Y是烷基，三卤代甲基，苯基，卤代苯基或烷基苯基。

5. 发明授权

US5360939A Homogeneous bimetallic hydroformylation catalysts, and processes utilizing these catalysts for conducting hydroformylation reactions 失效
标题翻译：均相双金属加氢甲酰化催化剂，以及利用这些催化剂进行加氢甲酰化反应的方法
公开(公告)号：US5360939A
公开(公告)日：1994-11-01
申请号：US180537
申请日：1994-01-12
申请人： George G. Stanley , Scott A. Laneman
发明人： George G. Stanley , Scott A. Laneman
IPC分类号： B01J31/24 , C07C29/141 , C07C45/49 , C07C45/50 , C07C51/14 , C07C67/293 , C07C253/10 , C07F9/50 , C07F15/00
CPC分类号： B01J31/1845 , B01J31/24 , B01J31/2409 , C07C29/141 , C07C45/49 , C07C45/50 , C07C45/505 , C07C51/14 , C07C67/293 , C07F15/0013 , C07F15/008 , C07F9/5027 , B01J2231/321 , B01J2531/0205 , B01J2531/10 , B01J2531/80 , B01J2531/822
摘要： Novel homogeneous bimetallic hydroformylation catalysts, and processes utilizing these catalysts to convert alkenes, particularly alpha olefins, under mild conditions to a product rich in aldehydes, particularly a product containing a high ratio of linear:branched chain aldehydes. The catalysts can be produced from a binucleating tetratertiaryphosphine ligand capable of strongly coordinating two metal centers and holding them in general proximity to one another. Bimetallic catalyst precursors are produced which, on reaction with carbon monoxide and hydrogen, form the active bimetallic hydroformylation catalyst system.
摘要翻译：新型均相双金属加氢甲酰化催化剂，以及利用这些催化剂将烯烃特别是α-烯烃在温和条件下转化成富含醛的产物，特别是含有高比例的直链支链醛的产物的方法。催化剂可以由能够强烈配位两个金属中心并将它们保持在彼此接近的双核四核膦配位体制备。制备双金属催化剂前体，其与一氧化碳和氢气反应形成活性双金属加氢甲酰化催化剂体系。

6. 发明授权

US5202473A Ruthenium-binap asymmetric hydrogenation catalyst 失效
标题翻译：钌 - 二元不对称氢化催化剂
公开(公告)号：US5202473A
公开(公告)日：1993-04-13
申请号：US917874
申请日：1992-07-23
申请人： Albert S. C. Chan , Scott A. Laneman
发明人： Albert S. C. Chan , Scott A. Laneman
IPC分类号： B01J31/24 , C07C45/46 , C07C51/15 , C07C51/36 , C07C51/377 , C07F15/00
CPC分类号： C07C51/36 , B01J31/2452 , C07C45/46 , C07C51/15 , C07C51/377 , C07F15/0053 , C07F15/008 , B01J2231/645 , B01J2531/0266 , B01J2531/821
摘要： A ruthenium-phosphine complex represented by the formula:[RuXY(BINAP].sub.nwherein n is an integer of from 1 to about 10; and X and Y independently represent nonchelating anionic ligands.
摘要翻译：由式[RuXY（BINAP）n表示的钌膦络合物，其中n为1至约10的整数; X和Y独立地表示非螯合的阴离子配体。

7. 发明授权

US5902904A Method for preparation of tertiary phosphines via nickel-catalyzed cross coupling 有权
标题翻译：通过镍催化交叉偶联制备叔膦的方法
公开(公告)号：US5902904A
公开(公告)日：1999-05-11
申请号：US138004
申请日：1998-08-21
申请人： Scott A. Laneman , David J. Ager , Amihia Eisenstadt
发明人： Scott A. Laneman , David J. Ager , Amihia Eisenstadt
IPC分类号： B01J31/26 , C07B61/00 , C07F9/50
CPC分类号： C07F9/5068
摘要： The invention is an improved method for the preparation of tertiary phosphines by way of cross-coupling of aryl, alkenyl, cycloalkenyl or aralkyl halides or aryl, alkenyl, cycloalkenyl or aralkyl sulfonate esters with chlorophosphines in the presence of a catalyst and a reductant. The general reaction scheme is shown below: ##STR1## wherein R.sup.1 is aryl, alkenyl, cycloalkenyl or aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl, or CONR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; R.sup.2 and R.sup.3 are independently aryl, alkyl, aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl or CONR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; and n is 2 where R.sup.1 is a difunctional moiety and 1 for any other R.sup.1 ; and X is Cl, Br, I, or OSO.sub.2 Y; wherein Y is alkyl, trihalomethyl, phenyl, halophenyl, or alkylphenyl.
摘要翻译：本发明是通过芳基，链烯基，环烯基或芳烷基卤化物或芳基，烯基，环烯基或芳烷基磺酸酯与氯膦在催化剂和还原剂存在下交叉偶联来制备叔膦的改进方法。一般反应方案如下所示：其中R1是芳基，烯基，环烯基或芳烷基，其中任何一个可以被一个或多个下列基团取代：烷基，芳基，芳烷基，烷氧基，烷酰基，氯，氟，烷氧基羰基，氰基，三氟甲基，环烷基或CONR 4 R 5，其中R 4和R 5独立地是氢，烷基，芳基或芳烷基; R 2和R 3独立地是芳基，烷基，芳烷基，其中任何一个可以被一个或多个下列基团取代：烷基，芳基，芳烷基，烷氧基，烷酰基，氯，氟，烷氧基羰基，氰基，三氟甲基，环烷基或CONR 4 R 5，其中R 4 和R 5独立地是氢，烷基，芳基或芳烷基; 并且n为2，其中R 1为双官能部分，1为任何其它R 1; X为Cl，Br，I或OSO 2 Y; 其中Y是烷基，三卤代甲基，苯基，卤代苯基或烷基苯基。

8. 发明授权

US5576447A Process for the preparation of amidino phenyl pyrrolidine .beta.-alanine urea analogs 失效
标题翻译：制备脒基苯基吡咯烷β-丙氨酸脲类似物的方法
公开(公告)号：US5576447A
公开(公告)日：1996-11-19
申请号：US465212
申请日：1995-06-05
申请人： Norman A. Abood , Daniel L. Flynn , Scott A. Laneman , Roger Nosal , Lori A. Schretzman
发明人： Norman A. Abood , Daniel L. Flynn , Scott A. Laneman , Roger Nosal , Lori A. Schretzman
IPC分类号： A61K31/40 , A61K31/4015 , A61P7/02 , C07C323/60 , C07D207/26 , C07D207/273
CPC分类号： C07D207/273
摘要： The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
摘要翻译：本发明涉及通过在碱存在下在合适的非质子溶剂中通过用三甲基锍卤化物或三甲基氧化锍卤化物处理甲硫氨酸类似物，从式IMA图谱的甲硫氨酸类似物制备式“的内酰胺的方法。本发明进一步涉及使用这种甲硫氨酸和内酰胺化合物作为中间体制备脒基苯基吡咯烷基β-丙氨酸脲类似物，β-丙氨酸脲类似物可用作抗血栓形成剂。

9. 发明授权

US5200539A Homogeneous bimetallic hydroformylation catalysts, and processes utilizing these catalysts for conducting hydroformylation reactions 失效
标题翻译：均相双金属加氢甲酰化催化剂，以及利用这些催化剂进行加氢甲酰化反应的方法
公开(公告)号：US5200539A
公开(公告)日：1993-04-06
申请号：US573355
申请日：1990-08-27
申请人： George G. Stanley , Scott A. Laneman
发明人： George G. Stanley , Scott A. Laneman
IPC分类号： B01J31/24 , C07C29/141 , C07C45/49 , C07C45/50 , C07C51/14 , C07C67/293 , C07C253/10 , C07F9/50 , C07F15/00
CPC分类号： B01J31/1845 , B01J31/24 , B01J31/2409 , C07C29/141 , C07C45/49 , C07C45/50 , C07C45/505 , C07C51/14 , C07C67/293 , C07F15/0013 , C07F15/008 , C07F9/5027 , B01J2231/321 , B01J2531/0205 , B01J2531/10 , B01J2531/80 , B01J2531/822
摘要： Novel homogeneous bimetallic hydroformylation catalysts, and processes utilizing these catalysts to convert alkenes, particularly alpha olefins, under mild conditions to a product rich in aldehydes, particularly a product containing a high ratio of linear:branched chain aldehydes. The catalysts can be produced from a binucleating tetratertiaryphosphine ligand capable of strongly coordinating two metal centers and holding them in general proximity to one another. Bimetallic catalyst precursors are produced which, on reaction with carbon monoxide and hydrogen forms the active bimetallic hydroformylation catalyst system.
摘要翻译：新型均相双金属加氢甲酰化催化剂，以及利用这些催化剂将烯烃特别是α-烯烃在温和条件下转化成富含醛的产物，特别是含有高比例的直链支链醛的产物的方法。催化剂可以由能够强烈配位两个金属中心并将它们保持在彼此接近的双核四核膦配位体制备。制备双金属催化剂前体，其与一氧化碳和氢气反应形成活性双金属加氢甲酰化催化剂体系。

10. 发明授权

US5198561A Ruthenium-BINAP asymmetric hydrogenation catalyst 失效
标题翻译：钌-BINAP不对称氢化催化剂
公开(公告)号：US5198561A
公开(公告)日：1993-03-30
申请号：US665069
申请日：1991-03-06
申请人： Albert S. C. Chan , Scott A. Laneman
发明人： Albert S. C. Chan , Scott A. Laneman
IPC分类号： B01J31/24 , C07C45/46 , C07C51/15 , C07C51/36 , C07C51/377 , C07F15/00
CPC分类号： C07C51/36 , B01J31/2452 , C07C45/46 , C07C51/15 , C07C51/377 , C07F15/0053 , C07F15/008 , B01J2231/645 , B01J2531/0266 , B01J2531/821
摘要： A ruthenium-phosphine complex represented by the formula:[RuXY(BINAP)].sub.nwherein n is an integer of from 1 to about 10; and X and Y independently represent nonchelating anionic ligands.
摘要翻译：由式[RuXY（BINAP）] n表示的钌膦络合物，其中n为1至约10的整数; X和Y独立地表示非螯合阴离子配位体。

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