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1. 发明申请

WO2009083899A3 PROCESS FOR THE PREPARATION OF AN ENANTIOMERIC TRISUBSTITUTED 3,4-DIHYDRO-ISOQUINOLINE DERIVATIVE 审中-公开
标题翻译：制备三羟甲基丙酮衍生物的方法
公开(公告)号：WO2009083899A3
公开(公告)日：2009-08-20
申请号：PCT/IB2008055504
申请日：2008-12-23
申请人： ACTELION PHARMACEUTICALS LTD , BAPPERT ERHARD , DE VRIES ANDREAS HENDRIKUS MAR , DOMIN DORIS , HELMS MATTHIAS , IMBODEN CHRISTOPH , NAZIR ZARGHUN , SKRANC WOLFGANG , SPINDLER FELIX , STANEK MICHAEL , TSCHEBULL WILHELM , VERZIJL GERARDUS KAREL MARIA
发明人： BAPPERT ERHARD , DE VRIES ANDREAS HENDRIKUS MARIA , DOMIN DORIS , HELMS MATTHIAS , IMBODEN CHRISTOPH , NAZIR ZARGHUN , SKRANC WOLFGANG , SPINDLER FELIX , STANEK MICHAEL , TSCHEBULL WILHELM , VERZIJL GERARDUS KAREL MARIA
IPC分类号： C07D217/02 , C07F17/02
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)-a-(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。

2. 发明申请

WO2009007460A3 ENANTIOSELECTIVE REDUCTION 审中-公开
标题翻译：增强选择性减少
公开(公告)号：WO2009007460A3
公开(公告)日：2009-04-02
申请号：PCT/EP2008059143
申请日：2008-07-11
申请人： DSM IP ASSETS BV , WILDEMAN DE STEFAAN MARIE ANDRE , STRAATMAN HENRICUS MARTINUS MARIA GERARDUS , VERZIJL GERARDUS KAREL MARIA , VERMOTE LINDA , VRIES DE ANDREAS HENDRIKUS MARIA
发明人： WILDEMAN DE STEFAAN MARIE ANDRE , STRAATMAN HENRICUS MARTINUS MARIA GERARDUS , VERZIJL GERARDUS KAREL MARIA , VERMOTE LINDA , VRIES DE ANDREAS HENDRIKUS MARIA
IPC分类号： C12P7/24 , C12P7/40 , C12P7/62 , C12P7/64 , C12P13/00 , C12P13/02 , C12P41/00
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 a,ß-unsaturated compound in a mixture comprising both an E isomer and a Z isomer of the a,ß-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，其包括在包含a，β不饱和键的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。

3. 发明申请

WO2003051827A1 PROCESS FOR THE PREPARATION OF AN ENANTIOMERICALLY ENRICHED THIO COMPOUND 审中-公开
标题翻译：制备完全有效的THIO化合物的方法
公开(公告)号：WO2003051827A1
公开(公告)日：2003-06-26
申请号：PCT/NL2002/000781
申请日：2002-12-02
申请人： DSM N.V. , KUILMAN, Thijs , BROXTERMAN, Quirinus, Bernardus , VERZIJL, Gerardus, Karel, Maria , STRAATMAN, Henricus, Martinus, Maria, Gerardus
发明人： KUILMAN, Thijs , BROXTERMAN, Quirinus, Bernardus , VERZIJL, Gerardus, Karel, Maria , STRAATMAN, Henricus, Martinus, Maria, Gerardus
IPC分类号： C07C327/32
CPC分类号： C07C327/32
摘要： The invention relates to a process for the preparation of an enantiomerically enriched compound of formula (1) or a salt thereof, in which R 1 and R 2 each independently represent an (hetero)alkyl or (hetero)aryl group, wherein R 1 -C(O)-SH or a salt thereof, with R 1 as defined above, is reacted with R 2 -C(C=CH 2 )-C(O)OH with R 2 as defined above, wherein the reaction takes place in the presence of catalyst is an enantiomerically enriched Lewis acid containing a transition metal chosen from the group of Ti, Zr and Hf or a combination thereof and at least one enantiomerically enriched ligand, and in the presence of an alkali metal ion, an alkaline earth metal ion or an ammonium ion.
摘要翻译：本发明涉及制备对映体富集的式（1）化合物或其盐的方法，其中R 1和R 2各自独立地表示（杂）烷基或（杂）芳基，其中R 1 -C（O）-SH或其与R 1如上所定义的盐与R 2 -C（C = CH 2）-C（O）OH与R 2反应其中所述反应在催化剂存在下进行，是含有选自Ti，Zr和Hf的过渡金属或其组合的对映体富集的路易斯酸和至少一种对映异构体富集的配体，并且在存在碱金属离子，碱土金属离子或铵离子。

4. 发明申请

WO2010010165A1 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：WO2010010165A1
公开(公告)日：2010-01-28
申请号：PCT/EP2009/059526
申请日：2009-07-23
申请人： DSM IP ASSETS BV , VRIES DE, Andreas, Hendrikus, Maria , VERZIJL, Gerardus, Karel, Maria , HERMSEN, Petrus, Johannes , CASTELIJNS, Anna, Maria, Cornelia, Francisca
发明人： VRIES DE, Andreas, Hendrikus, Maria , VERZIJL, Gerardus, Karel, Maria , HERMSEN, Petrus, Johannes , CASTELIJNS, Anna, Maria, Cornelia, Francisca
IPC分类号： C07D307/33 , C07D69/77 , C07C235/02
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。

5. 发明申请

WO2009083903A1 TRISUBSTITUTED 3,4-DIHYDRO-1H-ISOQUINOLIN COMPOUND, PROCESS FOR ITS PREPARATION, AND ITS USE 审中-公开
标题翻译：三取代3,4-二氢-1H-异喹啉化合物，其制备方法及其用途
公开(公告)号：WO2009083903A1
公开(公告)日：2009-07-09
申请号：PCT/IB2008/055509
申请日：2008-12-23
申请人： ACTELION PHARMACEUTICALS LTD , DE VRIES, Andreas, Hendrikus, Maria , DOMIN, Doris , HELMS, Matthias , IMBODEN, Christoph , KOBERSTEIN, Ralf , NAZIR, Zarghun , SKRANC, Wolfgang , STANEK, Michael , TSCHEBULL, Wilhelm , VERZIJL, Gerardus, Karel, Maria
发明人： DE VRIES, Andreas, Hendrikus, Maria , DOMIN, Doris , HELMS, Matthias , IMBODEN, Christoph , KOBERSTEIN, Ralf , NAZIR, Zarghun , SKRANC, Wolfgang , STANEK, Michael , TSCHEBULL, Wilhelm , VERZIJL, Gerardus, Karel, Maria
IPC分类号： C07D217/18 , A61K31/472
CPC分类号： C07D217/18
摘要： The present invention relates to the compound of formula (7*)acetate (see below), a process for its preparation, and its use.
摘要翻译：本发明涉及式（7 *）乙酸酯化合物（见下文），其制备方法及其应用。

6. 发明申请

WO2006050988A1 CHIRAL COMPOUND SUITABLE AS A CATALYST FOR ASYMMETRIC TRANSFER HYDROGENATION 审中-公开
标题翻译：适用于不对称转移氢化催化剂的CHIRAL COMPOUND
公开(公告)号：WO2006050988A1
公开(公告)日：2006-05-18
申请号：PCT/EP2005/012198
申请日：2005-11-10
申请人： DSM IP ASSETS B.V. , VRIES DE, Johannes, Gerardus , VERZIJL, Gerardus, Karel, Maria , VRIES DE, Andreas, Hendrikus, Maria , RITLENG, Vincent , VOELKLIN, Adeline, Marie, Josèphe
发明人： VRIES DE, Johannes, Gerardus , VERZIJL, Gerardus, Karel, Maria , VRIES DE, Andreas, Hendrikus, Maria , RITLENG, Vincent , VOELKLIN, Adeline, Marie, Josèphe
IPC分类号： C07F17/00
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s- 键合到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，其中M直接与所述二齿配位体的伯或仲氨基的氮原子结合，由此形成金属环在所述二齿配体和金属M之间，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。

7. 发明申请

WO2009083899A2 PROCESS FOR THE PREPARATION OF AN ENANTIOMERIC TRISUBSTITUTED 3,4-DIHYDRO-ISOQUINOLINE DERIVATIVE 审中-公开
标题翻译：制备三取代的三取代3,4-二氢 - 异喹啉衍生物的方法
公开(公告)号：WO2009083899A2
公开(公告)日：2009-07-09
申请号：PCT/IB2008/055504
申请日：2008-12-23
申请人： ACTELION PHARMACEUTICALS LTD , BAPPERT, Erhard , DE VRIES, Andreas, Hendrikus, Maria , DOMIN, Doris , HELMS, Matthias , IMBODEN, Christoph , NAZIR, Zarghun , SKRANC, Wolfgang , SPINDLER, Felix , STANEK, Michael , TSCHEBULL, Wilhelm , VERZIJL, Gerardus, Karel, Maria
发明人： BAPPERT, Erhard , DE VRIES, Andreas, Hendrikus, Maria , DOMIN, Doris , HELMS, Matthias , IMBODEN, Christoph , NAZIR, Zarghun , SKRANC, Wolfgang , SPINDLER, Felix , STANEK, Michael , TSCHEBULL, Wilhelm , VERZIJL, Gerardus, Karel, Maria
IPC分类号： C07D217/02 , C07F17/02
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-1-基] 铱]，（S）-1-二环己基膦基-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。

8. 发明申请

WO2009007461A1 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：WO2009007461A1
公开(公告)日：2009-01-15
申请号：PCT/EP2008/059144
申请日：2008-07-11
申请人： DSM IP ASSETS B.V. , VERZIJL, Gerardus, Karel, Maria , STRAATMAN, Henricus, Martinus, Maria, Gerardus , VRIES DE, Andreas, Hendrikus, Maria , SCHMIEDER, Lizette , BOOGERS, Jeroen, Antonius, Franciscus
发明人： VERZIJL, Gerardus, Karel, Maria , STRAATMAN, Henricus, Martinus, Maria, Gerardus , VRIES DE, Andreas, Hendrikus, Maria , SCHMIEDER, Lizette , BOOGERS, Jeroen, Antonius, Franciscus
IPC分类号： C07C47/277 , C07F7/18 , C12P7/24
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 R 1 , R 2 and R 5 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, R 1 and/or R 2 may be a cation, R 3 , and R 4 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 R 1 , R 2 , R 3 , R 4 and R 5 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. 发明申请

WO2005095629A1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY ENRICHED ESTERS AND ALCOHOLS BY MEANS OF AZEOTROPICALLY DRIED ENZYME COMPOSITIONS 审中-公开
标题翻译：通过亚硫酸酯酶组合物制备高效酯和醇的方法
公开(公告)号：WO2005095629A1
公开(公告)日：2005-10-13
申请号：PCT/EP2005/003312
申请日：2005-03-25
申请人： DSM IP ASSETS B.V. , VERZIJL, Gerardus, Karel, Maria
发明人： VERZIJL, Gerardus, Karel, Maria
IPC分类号： C12P41/00
CPC分类号： C12P41/004
摘要： Process for the preparation of an enantiomerically enriched ester, which comprises subjecting a mixture of enantiomers of the corresponding secondary alcohol, in the presence of an acyl donor, to an enantioselective enzymatic conversion, wherein the conversion is carried out by using a mixture containing an enantioselective acylating enzyme, which enzyme mixture is prepared by mixing an aqueous solution of the enantioselective acylating enzyme with an organic compound which forms an azeotrope with water and by subsequently azeotropically removing the water.
摘要翻译：制备对映异构体富集的酯的方法，其包括在酰基供体存在下使相应仲醇的对映异构体的混合物进行对映选择性酶转化，其中转化通过使用含有对映选择性的酰化酶，该酶混合物通过将对映选择性酰化酶的水溶液与与水形成共沸物的有机化合物和随后共沸除去水而制备。

10. 发明申请

WO2004046088A8 PROCESS FOR THE RACEMISATION OF ENANTIOMERICALLY ENRICHED ALPHA-AMINO NITRILES 审中-公开
标题翻译：高效液相色谱法制备高效液相色谱法
公开(公告)号：WO2004046088A8
公开(公告)日：2005-09-29
申请号：PCT/EP0312412
申请日：2003-11-03
申请人： DSM IP ASSETS BV , VERZIJL GERARDUS KAREL MARIA , BROXTERMAN QUIRINUS BERNARDUS
发明人： VERZIJL GERARDUS KAREL MARIA , KAPTEIN BERNARDUS , BROXTERMAN QUIRINUS BERNARDUS
IPC分类号： C07C253/30 , C07C255/24 , C07C255/42 , C07C255/44
CPC分类号： C07C253/30 , C07C255/24 , C07C255/42 , C07C255/44
摘要： Process for the racemisation of an enantiomerically enriched alpha-amino nitrile characterized in that the enantiomerically enriched alpha-amino nitrile is contacted with a lewis acid catalyst. Preferably an aprotic solvent is used. The lewis acid catalyst preferably comprises a metal chosen from main group elements IA-IVA of the Periodic Table (CAS version), the transition metals and the lanthanides, in particular Al, Ti, Zr, or lanthanides. The catalsyt for example has the general structure MnXpSqLr, and preferably is chosen from the group of aluminum alkoxides, aluminum alkyls, lanthanide alkoxydes and lanthanocenes. The racemisation may be performed in combination with a resolution process, for instance in combination with an enzymatic or a crystallization induced resolution process, preferably in situ, for instance in situ in a crystallization induced asymmetric transformation process.
摘要翻译：对映异构体富集的α-氨基腈的外消旋化方法，其特征在于对映异构体富集的α-氨基腈与路易斯酸催化剂接触。优选使用非质子溶剂。路易斯酸催化剂优选包含选自元素周期表主要元素IA-IVA（CAS版）的金属，过渡金属和镧系元素，特别是Al，Ti，Zr或镧系元素。例如，催化剂具有MnXpSqLr的一般结构，优选选自烷氧基铝，烷基铝，镧系烷氧基化物和镧系元素。外消旋化可以与分辨方法结合进行，例如与酶或结晶诱导的分辨方法组合进行，优选原位，例如在结晶诱导的非对称转化过程中原位。

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