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1. 发明授权

US07884223B2 Chiral compound suitable as a catalyst for asymmetric transfer hydrogenation 有权
标题翻译：适用于不对称转移氢化催化剂的手性化合物
公开(公告)号：US07884223B2
公开(公告)日：2011-02-08
申请号：US11667381
申请日：2005-11-10
申请人： Johannes Gerardus (Hans) De Vries , Gerardus Karel Maria Verzijl , Andreas Hendrikus Maria De Vries , Vincent Ritleng , Adeline Marie Joseèphe Voelklin
发明人： Johannes Gerardus (Hans) De Vries , Gerardus Karel Maria Verzijl , Andreas Hendrikus Maria De Vries , Vincent Ritleng , Adeline Marie Joseèphe Voelklin
IPC分类号： C07F15/00 , B01J31/00
CPC分类号： C07F17/02
摘要： The invention relates to an enantiomerically enriched chiral compound comprising a transition metal M, which comprises four, five or six coordinating groups of which at least one pair is linked together to form a bidentate ligand, in which M is directly bound via one single σ-bond to a carbon atom of an optionally substituted and/or optionally fused (hetero)aromatic ring of said bidentate ligand and in which M is directly bound to a nitrogen atom of a primary or secondary amino group of said bidentate ligand, thereby forming a metallacycle between said bidentate ligand and the metal M, said metal M being selected from the metals of groups 8 and 9 of the Periodic Table of the Elements, in particular iron, ruthenium, osmium, cobalt, rhodium, or iridium. The chiral compound can be used as a catalyst, preferably in an asymmetric transfer hydrogenation process. The invention further relates to a process for an asymmetric transfer hydrogenation of a prochiral compound in the presence of a hydrogen donor and the chiral compound of the invention comprising a transition metal chosen from the metals of groups 8, 9 and 10 of the Periodic Table, in particular iron, ruthenium, osmium, cobalt, rhodium, iridium, nickel, palladium or platinum as the catalyst.
摘要翻译：本发明涉及包含过渡金属M的对映异构体富集的手性化合物，其包含四个，五个或六个配位基团，其中至少一对连接在一起形成双齿配体，其中M通过一个单一的直接结合; 与所述二齿配位体的任选取代的和/或任选稠合的（杂）芳族环的碳原子键合，并且其中M直接键合到所述二齿配位体的伯或仲氨基的氮原子上，从而形成所述二齿配体和金属M之间的金属循环，所述金属M选自元素周期表第8和9族的金属，特别是铁，钌，锇，钴，铑或铱。手性化合物可以用作催化剂，优选在不对称转移氢化方法中。本发明还涉及在氢供体和含有选自元素周期表第8,9和10族的金属的过渡金属的本发明的手性化合物的存在下前手性化合物的不对称转移氢化的方法，特别是铁，钌，锇，钴，铑，铱，镍，钯或铂作为催化剂。

2. 发明申请

US20100305325A1 PROCESS FOR THE PREPARATION OF AN ENANTIOMERIC TRISUBSTITUTED 3,4-DIHYDRO-ISOQUINOLINE DERIVATIVE 有权
标题翻译：制备三羟甲基丙酮衍生物的方法
公开(公告)号：US20100305325A1
公开(公告)日：2010-12-02
申请号：US12810176
申请日：2008-12-23
申请人： Erhard Bappert , Andreas Hendrikus Maria De Vries , Doris Domin , Matthias Helms , Christoph Imboden , Zarghun Nazir , Wolfgang Skranc , Felix Spindler , Michael Stanek , Wilhelm Tschebull , Gerardus Karel Maria Verzijl
发明人： Erhard Bappert , Andreas Hendrikus Maria De Vries , Doris Domin , Matthias Helms , Christoph Imboden , Zarghun Nazir , Wolfgang Skranc , Felix Spindler , Michael Stanek , Wilhelm Tschebull , Gerardus Karel Maria Verzijl
IPC分类号： C07D217/20
CPC分类号： C07D217/02
摘要： The present invention relates to a process for the preparation of the compound of formula (7) which process comprises the hydrogenation of the compound of formula (4) using bis[chloro-1,5-cyclooctadiene-iridium], (S)-i-dicyclohexylphosphino-2-[(S)-α-(dimethylamino)-2-(dicyclohexylphosphino)benzyl]-ferrocene as a catalyst.
摘要翻译：本发明涉及制备式（7）化合物的方法，该方法包括使用双[氯-1,5-环辛二烯 - 铱]，（S）-i 二环己基膦基-2 - [（S）-α-（二甲基氨基）-2-（二环己基膦基）苄基] - 二茂铁作为催化剂。

3. 发明申请

US20130252288A1 ENANTIOSELECTIVE REDUCTION 审中-公开
标题翻译：增强选择性减少
公开(公告)号：US20130252288A1
公开(公告)日：2013-09-26
申请号：US12668082
申请日：2008-07-11
申请人： Stefaan Marie André De Wildeman , Henricus Martinus Maria Straatman , Gerardus Karel Maria Verzijl , Linda M. Vermote , Andreas Hendrikus Maria De Vries
发明人： Stefaan Marie André De Wildeman , Henricus Martinus Maria Straatman , Gerardus Karel Maria Verzijl , Linda M. Vermote , Andreas Hendrikus Maria De Vries
IPC分类号： C12P17/10 , C12P7/26 , C12P7/22 , C12P7/24
CPC分类号： C12P17/10 , C12P7/22 , C12P7/24 , C12P7/26 , C12P13/02 , C12P41/002
摘要： The invention relates to a process for the preparation of a chiral compound, comprising enantioselectively reducing a carbon-carbon double bond of an α,β-unsaturated compound in a mixture comprising both an E isomer and a Z isomer of the α,β-unsaturated compound, wherein both E isomer and Z isomer are converted in the presence of a hydrogenation catalyst.
摘要翻译：本发明涉及一种制备手性化合物的方法，包括在包含α，β-不饱和的E异构体和Z异构体的混合物的对映体选择性还原α，β-不饱和化合物的碳 - 碳双键化合物，其中E异构体和Z异构体在氢化催化剂存在下转化。

4. 发明授权

US08314238B2 Process for the preparation of an enantiomeric trisubstituted 3,4-dihydro-isoquinoline derivative 有权
标题翻译：制备对映体三取代3,4-二氢异喹啉衍生物的方法
公开(公告)号：US08314238B2
公开(公告)日：2012-11-20
申请号：US12810176
申请日：2008-12-23
申请人： Erhard Bappert , Andreas Hendrikus Maria De Vries , Doris Domin , Matthias Helms , Christoph Imboden , Zarghun Nazir , Wolfgang Skranc , Felix Spindler , Michael Stanek , Wilhelm Tschebull , Gerardus Karel Maria Verzijl
发明人： Erhard Bappert , Andreas Hendrikus Maria De Vries , Doris Domin , Matthias Helms , Christoph Imboden , Zarghun Nazir , Wolfgang Skranc , Felix Spindler , Michael Stanek , Wilhelm Tschebull , Gerardus Karel Maria Verzijl
IPC分类号： C07D217/20 , A61K31/47
CPC分类号： C07D217/02
摘要： The present invention relates to a process for the preparation of the compound of formula (7) which process comprises the hydrogenation of the compound of formula (4) using bis[chloro-1,5-cyclooctadiene-iridium], (S)-i-dicyclohexylphosphino-2-[(S)-α-(dimethylamino)-2-(dicyclohexylphosphino)benzyl]-ferrocene as a catalyst.
摘要翻译：本发明涉及制备式（7）化合物的方法，该方法包括使用双[氯-1,5-环辛二烯 - 铱]，（S）-i 二环己基膦基-2 - [（S）-α-（二甲基氨基）-2-（二环己基膦基）苄基] - 二茂铁作为催化剂。

5. 发明授权

US08088954B2 Preparation of a saturated aldehyde 失效
标题翻译：制备饱和醛
公开(公告)号：US08088954B2
公开(公告)日：2012-01-03
申请号：US12668232
申请日：2008-07-11
申请人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
发明人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
IPC分类号： C07C47/105 , C07C45/67 , C07C41/18
CPC分类号： C07C47/277 , C07C37/002 , C07C37/62 , C07C41/22 , C07C41/26 , C07C45/562 , C07C45/62 , C07C47/27 , C07C69/78 , C07C309/73 , C12P7/04 , C12P7/24 , C07C43/23 , C07C43/225 , C07C39/373 , C07C39/24 , C07C39/11
摘要： The invention relates to a compound according to Formula (IX) and salts thereof, wherein R1, R2 and R5 are each independently selected from H and hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, or when the compound according to formula (IX) is a salt, R1 and/or R2 may be a cation, R3, and R4 each independently selected from hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, and wherein any two of R1, R2, R3, R4 and R5 are optionally linked together to form a ring structure. The invention further relates to the preparation of such a compound and to the use of such a compound for preparing a pharmaceutical compound, an agrochemical compound, an intermediate for a pharmaceutical compound or an intermediate for an agrochemical compound.
摘要翻译：本发明涉及式（IX）化合物及其盐，其中R 1，R 2和R 5各自独立地选自H和烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基，或当式（IX）化合物为盐时，R 1和/或R 2可以是阳离子，R 3和R 4各自独立地选自烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基并且其中R 1，R 2，R 3，R 4和R 5中的任何两个任选地连接在一起以形成环结构。本发明还涉及这种化合物的制备以及这种化合物用于制备药物化合物，农药化合物，药物化合物的中间体或农药化合物的中间体的用途。

6. 发明申请

US20110294171A1 PREPARATION OF A SATURATED ALDEHYDE 审中-公开
标题翻译：饱和阿尔德的制备
公开(公告)号：US20110294171A1
公开(公告)日：2011-12-01
申请号：US13205442
申请日：2011-08-08
申请人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
发明人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
IPC分类号： C12P13/02 , C07C41/01 , C07C237/20 , C07C45/61 , C12P7/24 , C12P7/02
CPC分类号： C07C47/277 , C07C37/002 , C07C37/62 , C07C41/22 , C07C41/26 , C07C45/562 , C07C45/62 , C07C47/27 , C07C69/78 , C07C309/73 , C12P7/04 , C12P7/24 , C07C43/23 , C07C43/225 , C07C39/373 , C07C39/24 , C07C39/11
摘要： The invention relates to a compound according to Formula (IX) and salts thereof, wherein R1, R2 and R5 are each independently selected from H and hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, or when the compound according to formula (IX) is a salt, R1 and/or R2 may be a cation, R3, and R4 each independently selected from hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, and wherein any two of R1, R2, R3, R4 and R5 are optionally linked together to form a ring structure. The invention further relates to the preparation of such a compound and to the use of such a compound for preparing a pharmaceutical compound, an agrochemical compound, an intermediate for a pharmaceutical compound or an intermediate for an agrochemical compound.
摘要翻译：本发明涉及式（IX）化合物及其盐，其中R 1，R 2和R 5各自独立地选自H和烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基，或当式（IX）化合物为盐时，R 1和/或R 2可以是阳离子，R 3和R 4各自独立地选自烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基并且其中R 1，R 2，R 3，R 4和R 5中的任何两个任选地连接在一起以形成环结构。本发明还涉及这种化合物的制备以及这种化合物用于制备药物化合物，农药化合物，药物化合物的中间体或农药化合物的中间体的用途。

7. 发明申请

US20110244531A1 SYNTHESIS ROUTES TO 2(S),4(S),5(S),7(S)-2,7-DIALKYL-4-HYDROXY-5-AMINO-8-ARYL-OCTANOYL AMIDES 审中-公开
标题翻译：合成路线2（S），4（S），5（S），7（S）-2,7-二甲基-4-羟基-5-氨基-8-芳基 - 十八烷基酰胺
公开(公告)号：US20110244531A1
公开(公告)日：2011-10-06
申请号：US13055572
申请日：2009-07-23
申请人： Andreas Hendrikus Maria De Vries , Gerardus Karel Maria Verzijl , Petrus Johannes Hermsen , Anna Maria Cornelia Francisca Castelijns
发明人： Andreas Hendrikus Maria De Vries , Gerardus Karel Maria Verzijl , Petrus Johannes Hermsen , Anna Maria Cornelia Francisca Castelijns
IPC分类号： C12P17/04 , C07D307/33 , C12P13/02 , C12P13/00 , C07C237/20 , C07C237/22 , C07C235/78 , C07C231/12
CPC分类号： C07D307/33 , C07C227/04 , C07C227/06 , C07C231/02 , C07C231/12 , C07C251/16 , C07C229/34 , C07C237/20
摘要： The invention relates to a process for the preparation of compounds that are important building blocks in convergent synthesis routes to 2(S),4(S),5(S),7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amides or pharmaceutically acceptable salts thereof, such as the compound Aliskiren, and to a process for the preparation of these octanoyl amides, comprising reacting said building block.
摘要翻译：本发明涉及一种制备化合物的方法，其是在2（S），4（S），5（S），7（S）-2,7-二烷基-4-羟基 -5-氨基-8-芳基 - 辛酰基酰胺或其药学上可接受的盐，例如化合物阿利吉仑，以及制备这些辛酰基酰胺的方法，包括使所述结构单元反应。

8. 发明申请

US20100197972A1 PREPARATION OF A SATURATED ALDEHYDE 失效
标题翻译：饱和阿尔德的制备
公开(公告)号：US20100197972A1
公开(公告)日：2010-08-05
申请号：US12668232
申请日：2008-07-11
申请人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
发明人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
IPC分类号： C07C47/105 , C07C45/67 , C12P7/24 , C07C41/18 , C07C41/22
CPC分类号： C07C47/277 , C07C37/002 , C07C37/62 , C07C41/22 , C07C41/26 , C07C45/562 , C07C45/62 , C07C47/27 , C07C69/78 , C07C309/73 , C12P7/04 , C12P7/24 , C07C43/23 , C07C43/225 , C07C39/373 , C07C39/24 , C07C39/11
摘要： The invention relates to a compound according to Formula (IX) and salts thereof, wherein R1, R2 and R5 are each independently selected from H and hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, or when the compound according to formula (IX) is a salt, R1 and/or R2 may be a cation, R3, and R4 each independently selected from hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, and wherein any two of R1, R2, R3, R4 and R5 are optionally linked together to form a ring structure. The invention further relates to the preparation of such a compound and to the use of such a compound for preparing a pharmaceutical compound, an agrochemical compound, an intermediate for a pharmaceutical compound or an intermediate for an agrochemical compound.
摘要翻译：本发明涉及式（IX）化合物及其盐，其中R 1，R 2和R 5各自独立地选自H和烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基，或当式（IX）化合物为盐时，R 1和/或R 2可以是阳离子，R 3和R 4各自独立地选自烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基并且其中R 1，R 2，R 3，R 4和R 5中的任何两个任选地连接在一起以形成环结构。本发明还涉及这种化合物的制备以及这种化合物用于制备药物化合物，农药化合物，药物化合物的中间体或农药化合物的中间体的用途。

9. 发明授权

US09139515B2 Synthesis of R-biphenylalaninol 有权
标题翻译： R-联苯丙氨醇的合成
公开(公告)号：US09139515B2
公开(公告)日：2015-09-22
申请号：US14236999
申请日：2012-08-16
申请人： Petrus Johannes Hermsen , Peter Hans Ermann , Peter Hans Riebel , Michael Wolberg , Andreas Hendrikus Maria De Vries
发明人： Petrus Johannes Hermsen , Peter Hans Ermann , Peter Hans Riebel , Michael Wolberg , Andreas Hendrikus Maria De Vries
IPC分类号： C07C233/51 , C07C231/02 , C07C235/26 , C07C269/04 , C07C271/16 , C07C213/02 , C07C215/28 , C07C231/12 , C07C233/73 , C07C233/87
CPC分类号： C07C233/51 , C07C213/02 , C07C215/28 , C07C231/12 , C07C233/73 , C07C233/87 , C07C269/04 , C07C271/16
摘要： This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The invention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.
摘要翻译：本发明涉及一种用于合成R-联苯基苯丙醇和在本发明方法中形成的中间体化合物的新方法，即用于合成R-联苯丙氨醇的新型中间体。本发明还涉及R-联苯基丙氨醇。根据本发明的方法，R-联苯基苯丙醇和R-联苯丙氨醇的中间体都可用于药物活性化合物的合成。

10. 发明授权

US08088955B2 Alpha-substituted α,β-unsaturated E- or Z-aldehydes, use thereof, and processes for their preparation α,β 失效
标题翻译： α-取代的α，β-不饱和的E-或Z-醛，其用途及其制备方法α，bgr;
公开(公告)号：US08088955B2
公开(公告)日：2012-01-03
申请号：US12668236
申请日：2008-07-11
申请人： Gerhard Steinbauer , Martina Kotthaus , Klaus Edegger , Stefaan Marie Andre De Wildeman , Henricus Martinus Maria Gerardus Straatman , Anna Maria Cornelia Francisca Castelijns , Andreas Hendrikus Maria De Vries
发明人： Gerhard Steinbauer , Martina Kotthaus , Klaus Edegger , Stefaan Marie Andre De Wildeman , Henricus Martinus Maria Gerardus Straatman , Anna Maria Cornelia Francisca Castelijns , Andreas Hendrikus Maria De Vries
IPC分类号： C07C47/27 , C07C45/00 , C07C309/01 , C07F7/02
CPC分类号： C07C47/277 , C07C37/002 , C07C37/62 , C07C41/22 , C07C41/26 , C07C45/516 , C07C45/562 , C07C45/62 , C07C45/63 , C07C45/72 , C07C45/74 , C07C47/27 , C07C69/78 , C07C309/66 , C07C309/73 , C12P7/24 , C07C43/23 , C07C43/225 , C07C39/373 , C07C39/24
摘要： This invention relates to novel alpha-substituted α,β-unsaturated E- or Z-aldehydes, or isomer mixture thereof, of the formula (I) in which R1 and R2 may be identical or different and are each H or a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms and R3 and R4 may be identical or different and are each a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms, and R5 may be identical or different and is H or a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms, to the use thereof, and to processes for their preparation. The invention further relates to the preparation of further intermediates for pharmaceuticals and to the preparation of the pharmaceuticals.
摘要翻译：本发明涉及式（I）的新型α-取代的α，β-不饱和的E-或Z-醛或其异构体混合物，其中R 1和R 2可以相同或不同并且各自为H或烃，其中烃可以具有一个或多个杂原子，并且R 3和R 4可以相同或不同，并且各自为烃，其中烃可以具有一个或多个杂原子，R 5可以相同或不同，为H或烃，其中烃可以具有一个或多个杂原子，其用途及其制备方法。本发明还涉及药物的其它中间体的制备和药物的制备。

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