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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

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。

4. 发明申请

WO2006105996A3 PROCESS FOR THE PREPARATION OF AN OPTICALLY ACTIVE ESTER 审中-公开
标题翻译：制备光学活性酯的方法
公开(公告)号：WO2006105996A3
公开(公告)日：2006-12-21
申请号：PCT/EP2006003479
申请日：2006-04-06
申请人： DSM IP ASSETS BV , HEISE ANDREAS , VERZIJL GERARDUS KAREL MARIA , RABANI GOUHER , PALMANS ANJA RITA ALBERTA , HILKER IRIS
发明人： HEISE ANDREAS , VERZIJL GERARDUS KAREL MARIA , RABANI GOUHER , PALMANS ANJA RITA ALBERTA , HILKER IRIS
IPC分类号： C07B55/00 , C07C29/09 , C07C29/143 , C07C29/56 , C07C67/03 , C07C67/465 , C12P41/00
CPC分类号： C08G63/16 , C07B2200/07 , C07C29/1285 , C07C29/143 , C07C67/03 , C08G63/82 , C12P7/625 , C12P41/004 , C07C69/007 , C07C69/28 , C07C33/26
摘要： The invention relates to a process for the preparation of an optically active compound from raw materials comprising a di-ester and a chiral hydroxy- compound according to formula (I), wherein: R 1 , R 2 , R 4 and R 5 each independently represent hydrogen or an alkyl group with 1-20 C-atoms, an alkenyl group with 2-20 C-atoms, an alkynyl group with 2-20 C- atoms, or an (hetero)aryl group with 4-20 C-atoms optionally containing one or more O, S or N atoms, R 3 represents an alkyl group with 1-20 C-atoms, an alkenyl group with 2-20 C- atoms, an alkynyl group with 2-20 C-atoms, or an (hetero)aryl group with 4-20 C- atoms optionally containing one or more O, S or N atoms, the compound according to formula (I) comprises at least one chiral centre that has an a-carbon relative to a secondary hydroxy group, comprising the steps of a) bringing the di-ester, optionally a solvent, and the chiral hydroxy-compound according to formula (I) together to form a reaction system; b) adding an asymmetric transesterification catalyst, a racemisation catalyst and optionally a racemisation catalyst re-activating compound to the reaction system; c) bringing the reaction system to conditions where racemisation and enantioselective transesterefication take place, whereby the optically active compound is formed, whereby steps a), b) and c) may be executed sequentially or simultaneously, and whereby the chiral hydroxy-compound according to formula (I) may in step a) be partially or wholly replaced by the combination of the corresponding ketone and a reducing agent.
摘要翻译：本发明涉及一种由包含二酯和式（I）的手性羟基化合物的原料制备光学活性化合物的方法，其中：R 1，R 2 R 2，R 4和R 5各自独立地表示氢或具有1-20个C原子的烷基，具有2-20C的链烯基原子，具有2-20个C原子的炔基或具有任选含有一个或多个O，S或N原子的4-20个C原子的（杂）芳基，R 3表示具有1-20个C原子的烷基，具有2-20个C原子的烯基，具有2-20个C原子的炔基或具有4-20个C-原子的（杂）芳基，任选地含有一个或更多的O，S或N原子，根据式（I）的化合物包含相对于仲羟基具有a-碳的至少一个手性中心，包括以下步骤：a）将二酯，任选地溶剂和根据式（I）的手性羟基化合物一起形成反应体系; b）向反应体系中加入不对称酯交换催化剂，外消旋化催化剂和任选的外消旋催化剂再活化化合物; c）使反应体系进行发生外消旋化和对映选择性转移反应的条件，从而形成光学活性化合物，由此可以顺序或同时地进行步骤a），b）和c），由此根据式（I）可以在步骤a）中被相应的酮和还原剂的组合部分或全部代替。

5. 发明申请

WO03043575A2 PROCESS FOR THE SYNTHESIS OF (R)-1-(3,5-BIS(TRIFLUOROMETHYL)-PHENYL)ETHAN-1-OL AND ESTERS THEREOF BY DYNAMIC KINETIC RESOLUTION 审中-公开
标题翻译：（R）-1-（3,5-BIS（三氟甲基） - 苯基）合成的方法ETHAN-1-OL及其动力学动力学分解
公开(公告)号：WO03043575A2
公开(公告)日：2003-05-30
申请号：PCT/US0236969
申请日：2002-11-15
申请人： MERCK & CO INC , BROXTERMAN QUIRINUS BERNARDUS , VERZIJL GERARDUS KAREL MARIA
发明人： BROXTERMAN QUIRINUS BERNARDUS , VERZIJL GERARDUS KAREL MARIA
IPC分类号： C07C17/12 , C07C29/09 , C07C29/143 , C07C29/56 , C07C45/00 , C07C69/007 , C07C69/63 , C12P7/62 , C12P41/00 , A61K
CPC分类号： C07C17/12 , C07C29/095 , C07C29/143 , C07C29/56 , C07C29/92 , C07C45/004 , C07C69/007 , C07C69/63 , C12P7/62 , C12P41/004 , C07C25/13 , C07C49/80 , C07C33/46
摘要： The present invention is concerned with novel processes for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol and esters thereof via dynamic kinetic resolution. These compounds are useful as intermediates in the synthesis of compounds which possess pharmacological activity.
摘要翻译：本发明涉及通过动态动力学拆分制备（R）-1-（3,5-双（三氟甲基）苯基）乙-1-醇及其酯的新方法。这些化合物可用作合成具有药理活性的化合物的中间体。

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