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1. 发明申请

WO2013026773A1 SYNTHESIS OF R-BIPHENYLALANINOL 审中-公开
标题翻译： R-BIPHENYLALANINOL的合成
公开(公告)号：WO2013026773A1
公开(公告)日：2013-02-28
申请号：PCT/EP2012/066038
申请日：2012-08-16
申请人： DSM IP Assets B.V. , HERMSEN, Petrus Johannes , RIEBEL, Peter Hans , WOLBERG, Michael , VRIES DE, Andreas Hendrikus Maria , ERMANN, Peter Hans , DSM Fine Chemicals Austria Nfg. GmbH & Co KG
发明人： HERMSEN, Petrus Johannes , RIEBEL, Peter Hans , WOLBERG, Michael , VRIES DE, Andreas Hendrikus Maria , ERMANN, Peter Hans
IPC分类号： C07C235/26 , C07C231/02 , C07C231/18 , C07C215/20 , C07C213/08
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合成药物活性化合物。

2. 发明申请

WO2005118794A2 IMPROVED 2-DEOXY-D-RIBOSE 5-PHOSPHATE ALDOLASES FOR, AND USE IN PRODUCTION OF 2, 4, 6-TRIDEOXYHESOSES AND 6-HALO- OR 6-CYANO-SUBSTITUTED DERIVATIVES THEREOF 审中-公开
标题翻译：改进的2-脱氧-D-呋喃五磷酸酯，用于生产2,4,6-三磷酸和其中6-取代或6-取代的衍生物。
公开(公告)号：WO2005118794A2
公开(公告)日：2005-12-15
申请号：PCT/EP2005/005989
申请日：2005-06-02
申请人： DSM IP ASSETS B.V. , JENNEWEIN, Stefan, Martin , SCHUERMANN, Martin , MOMMERS, Johannes, Helena, Michael , MINK, Daniel , WOLBERG, Michael , WUBBOLTS, Marcel, Gerhardus
发明人： JENNEWEIN, Stefan, Martin , SCHUERMANN, Martin , MOMMERS, Johannes, Helena, Michael , MINK, Daniel , WOLBERG, Michael , WUBBOLTS, Marcel, Gerhardus
IPC分类号： C12N9/00
CPC分类号： C12N9/88 , C12P19/02
摘要： The invention relates to isolated mutants of enzymes from the group of 2-deoxy-D-ribose 5-phosphate aldolase wild-type enzymes having a productivity factor (as determined by a specific test) which is at least 10% higher than the productivity factor for the corresponding wild-type enzyme from which it is a mutant. The mutants have at least one amino acid substitution at one or more of the positions corresponding to K13, T19, Y49, N80, D84, A93, E127, A128, K146, K160,1166, A174, M185, K196, F200, and S239 in Escherichia coli K12 (EC 4.1.2.4) wild-type enzyme sequence, and/or a deletion of at least one amino acid at the positions corresponding to S258 and Y259 therein, optionally combined with, specific, C-terminal extension and/or N terminal extension. The invention also relates to screening processes to find 2-deoxy-D-ribose 5-phosphate aldolase enzymes (either as such or as mutants) having a productivity factor (as determined by said specific test, which forms an essential part of the screening) which is at least 10% higher than the reference value. Moreover, the invention relates to mutant enzymes obtained by the screening process, and to nucleic acids encoding such mutants, and to vectors and host cells comprising, respectively, such nucleic acids or mutants. Finally the invention relates to the use of such (preferably mutant) enzymes, nucleic acids, vectors and host cells in the production of, for instance, 6-chloro-2,4,6-trideoxyD-erythrohexapyranoside.
摘要翻译：本发明涉及分离的2-脱氧-D-核糖5-磷酸醛缩酶野生型酶的突变体，其具有比生产率高至少高10％的生产率因子（通过特异性测试确定）对于其为突变体的相应野生型酶。突变体在对应于K13，T19，Y49，N80，D84，A93，E127，A128，K146，K160,1166，A174，M185，K196，F200和S239的一个或多个位置具有至少一个氨基酸取代在大肠杆菌K12（EC 4.1.2.4）野生型酶序列中，和/或在其对应于S258和Y259的位置上的至少一个氨基酸的缺失，任选地与特异性C末端延伸和/或 N终端扩展。本发明还涉及筛选方法以找到具有生产率因子的2-脱氧-D-核糖-5-磷酸醛缩酶（或者作为突变体）（通过所述具体试验确定，其形成筛选的重要部分）其比参考值高至少10％。此外，本发明涉及通过筛选方法获得的突变酶，以及编码这种突变体的核酸，以及分别含有这些核酸或突变体的载体和宿主细胞。最后，本发明涉及这种（优选突变的）酶，核酸，载体和宿主细胞在生产例如6-氯-2,4,6-三脱氧-D-赤藓糖苷中的用途。

3. 发明申请

WO2011002999A1 SYNTHESIS OF N4- (2, 2-DIMETHYL-4- [ (DIHYDROGEN PHOSPHONOXY ] -3-OXO-5-PYRIDO [1, 4] OXAZIN-6-YL)-5-FLUORO-N2- (3, 4, 5,-TRIMETHOXYPHENYL) -2, 4- PYRIMIDINEDIAMINE DISODIUM SALT 审中-公开
标题翻译：合成N4-（2,2-二甲基-4 - [（二氢苯基）苯氧基] -3-氧代-5-吡啶并[1,4]氧杂-6-基）-5-氟-N 2 - （3,4,5 ， - 二甲苯基）-2,4-二吡啶二胺盐
公开(公告)号：WO2011002999A1
公开(公告)日：2011-01-06
申请号：PCT/US2010/040792
申请日：2010-07-01
申请人： RIGEL PHARMACEUTICALS, INC. , FELFER, Ulfried , GISELBRECHT, Karl-Heinz , WOLBERG, Michael
发明人： FELFER, Ulfried , GISELBRECHT, Karl-Heinz , WOLBERG, Michael
IPC分类号： C07F9/6561
CPC分类号： C07F9/091 , C07F9/6561
摘要： This invention relates to the field of pharmaceutical/process chemistry. Disclosed herein is a process for preparing N4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy) methyl] -3-oxo-5-pyrido [1,4] oxazin-6-yl) -5~fluoro-N2- (3,4, 5-trimethox yphenyl) -2, 4-pyrimidinediamine disodium salt, particularly hydrates (such as a hexahydrate). The compound is useful in the treatment and prevention of various diseases. Also disclosed is a process of preparing N4- (2, 2-dimethyl-4- [ (dialkyl phosphonoxy) methyl] -3-oxo-5-pyrido [1, 4] oxazin-6-yl) -5-f luoro-N2- (3,4, 5-trimethox yphenyl ) -2, 4-pyrimidinediamine. Both processes involve the use of an amide. in.
摘要翻译：本发明涉及药物/工艺化学领域。本文公开了制备N4-（2,2-二甲基-4 - [（二氢膦氧基）甲基] -3-氧代-5-吡啶并[1,4]恶嗪-6-基）-5-氟-N 2 - （3,4,5-三甲氧基苯基）-2,4-嘧啶二胺二钠盐，特别是水合物（例如六水合物）。该化合物可用于治疗和预防各种疾病。还公开了制备N4-（2,2-二甲基-4 - [（二烷基膦氧基）甲基] -3-氧代-5-吡啶并[1,4]恶嗪-6-基）-5-氟 - N2-（3,4,5-三甲氧基苯基）-2,4-嘧啶二胺。这两个方法涉及使用酰胺。在。

4. 发明申请

WO2005118794A3 IMPROVED 2-DEOXY-D-RIBOSE 5-PHOSPHATE ALDOLASES (DERAS) AND THE USES THEREOF 审中-公开
标题翻译：改进的2-脱氧-D-呋喃五磷酸酯（DERAS）及其用途
公开(公告)号：WO2005118794A3
公开(公告)日：2006-02-16
申请号：PCT/EP2005005989
申请日：2005-06-02
申请人： DSM IP ASSETS BV , JENNEWEIN STEFAN MARTIN , SCHUERMANN MARTIN , MOMMERS JOHANNES HELENA MICHAE , MINK DANIEL , WOLBERG MICHAEL , WUBBOLTS MARCEL GERHARDUS
发明人： JENNEWEIN STEFAN MARTIN , SCHUERMANN MARTIN , MOMMERS JOHANNES HELENA MICHAE , MINK DANIEL , WOLBERG MICHAEL , WUBBOLTS MARCEL GERHARDUS
IPC分类号： C12N15/60 , C12N9/88 , C12P19/02
CPC分类号： C12N9/88 , C12P19/02
摘要： The invention relates to isolated mutants of enzymes from the group of 2-deoxy-D-ribose 5-phosphate aldolase wild-type enzymes having a productivity factor (as determined by a specific test) which is at least 10% higher than the productivity factor for the corresponding wild-type enzyme from which it is a mutant. The mutants have at least one amino acid substitution at one or more of the positions corresponding to K13, T19, Y49, N80, D84, A93, E127, A128, K146, K160,1166, A174, M185, K196, F200, and S239 in Escherichia coli K12 (EC 4.1.2.4) wild-type enzyme sequence, and/or a deletion of at least one amino acid at the positions corresponding to S258 and Y259 therein, optionally combined with, specific, C-terminal extension and/or N terminal extension. The invention also relates to screening processes to find 2-deoxy-D-ribose 5-phosphate aldolase enzymes (either as such or as mutants) having a productivity factor (as determined by said specific test, which forms an essential part of the screening) which is at least 10% higher than the reference value. Moreover, the invention relates to mutant enzymes obtained by the screening process, and to nucleic acids encoding such mutants, and to vectors and host cells comprising, respectively, such nucleic acids or mutants. Finally the invention relates to the use of such (preferably mutant) enzymes, nucleic acids, vectors and host cells in the production of, for instance, 6-chloro-2,4,6-trideoxyD-erythrohexapyranoside.
摘要翻译：本发明涉及分离的2-脱氧-D-核糖5-磷酸醛缩酶野生型酶的突变体，其具有比生产率高至少高10％的生产率因子（通过特异性测试确定）对于其为突变体的相应野生型酶。突变体在对应于K13，T19，Y49，N80，D84，A93，E127，A128，K146，K160,1166，A174，M185，K196，F200和S239的一个或多个位置具有至少一个氨基酸取代在大肠杆菌K12（EC 4.1.2.4）野生型酶序列中，和/或在其对应于S258和Y259的位置上的至少一个氨基酸的缺失，任选地与特异性C末端延伸和/或 N终端扩展。本发明还涉及筛选方法以找到具有生产率因子的2-脱氧-D-核糖-5-磷酸醛缩酶（或者作为突变体）（通过所述具体试验确定，其形成筛选的重要部分）其比参考值高至少10％。此外，本发明涉及通过筛选方法获得的突变酶，以及编码这种突变体的核酸，以及分别含有这些核酸或突变体的载体和宿主细胞。最后，本发明涉及这种（优选突变的）酶，核酸，载体和宿主细胞在生产例如6-氯-2,4,6-三脱氧-D-赤藓糖苷中的用途。

5. 发明申请

WO2004096788A1 PROCESS FOT THE PREPARATION OF (4-HYDROXY-6-OXO-TETRAHYDROPYRAN-2-YL) ACETONITRILE AND DERIVATIVES THEREOF 审中-公开
标题翻译：方法制备（4-羟基-6-氧代 - 四氢吡喃-2-基）乙酸酯及其衍生物
公开(公告)号：WO2004096788A1
公开(公告)日：2004-11-11
申请号：PCT/NL2004/000284
申请日：2004-04-28
申请人： DSM IP ASSETS B.V. , MINK, Daniel , WOLBERG, Michael , BOESTEN, Wilhelmus, Hubertus, Joseph , SEREINIG, Natascha
发明人： MINK, Daniel , WOLBERG, Michael , BOESTEN, Wilhelmus, Hubertus, Joseph , SEREINIG, Natascha
IPC分类号： C07D309/00
CPC分类号： C07D309/30
摘要： The invention relates to a process for the preparation of (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile from 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one, wherein X stands for a leaving group, by reacting 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one with a cyanide ion in water and by subsequent lowering of the pH to a pH between 0 and 5. (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable from (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile may suitably be used in the preparation of a pharmaceutical preparation, more in particular in the preparation of statins, more in particular in the preparation of Atorvastatine or a salt thereof, for instance its calcium salt. The invention also relates to (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable therefrom.
摘要翻译：本发明涉及从6-X取代的甲基-4-羟基 - 四氢 - 吡喃-2-酮制备（4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙腈的方法，其中X代表离去基团，通过使6-X取代的甲基-4-羟基 - 四氢 - 吡喃-2-酮与氰化物离子在水中反应，随后将pH降低至0至5之间的pH。（4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙腈和从（4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙腈获得的其它化合物可适当地用于制备药物制剂，更特别是制备他汀类药物，更特别是制备阿托伐他汀或其盐，例如其钙盐。本发明还涉及（4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙腈及其可得的其它化合物。

6. 发明申请

WO2003027092A1 VERFAHREN ZUR TRENNUNG DIASTEREOMERER 1, 3-DIOL-ACETALE 审中-公开
标题翻译：法分离非对映体1，3-DIOL缩醛的
公开(公告)号：WO2003027092A1
公开(公告)日：2003-04-03
申请号：PCT/DE2002/002798
申请日：2002-07-31
申请人： FORSCHUNGSZENTRUM JÜLICH GMBH , BODE, Silke , WOLBERG, Michael , MÜLLER, Michael
发明人： BODE, Silke , WOLBERG, Michael , MÜLLER, Michael
IPC分类号： C07D319/06
CPC分类号： C07D319/06
摘要： Nach dem Stand der Technik ist die Trennung diastereomerer 1,3-Diole bzw. der entsprechenden 1,3-Diol-Acetale oder von syn - und anti -1,3-Diolen nach der allgemeinen Formel (I) bzw. (II) nur mit hohem technischen Aufwand unter Verlusten der gewünschten Produkte möglich. Mit dem erfindungsgemässen Verfahren zur Trennung diastereomerer 1/3-Diol-Acetale, bei dem eine partielle Hydrolyse des Gemisches dieser Verbindungen durchgeführt wird, ist es nunmehr möglich mit einfachen Methoden diese voneinander mit einer hohen Produktausbeute zu trennen und damit eine vereinfachte Methode zur Bereitstellung von Ausgangsverbindungen zur Synthese von z. B. syn - und anti - konfigurierten 3,5-Dihydroxy-carboxylaten zur Verfügung zu stellen.
摘要翻译：根据现有技术中，非对映体1,3-二醇或相应的1,3-二醇或通式（I）或（II）的顺式和反-1,3-二醇的缩醛的分离是唯一可能与期望的产品的损失大的技术努力。对于非对映异构第三二醇缩醛，其中这些化合物的混合物的部分水解进行的分离本发明的方法，现在有可能用简单的方法将它们彼此具有高的产品产率分离，并且由此简化方法，用于提供起始z的合成化合物。提供作为顺式和反配置3,5-二羟基羧酸盐是可用的。

7. 发明申请

WO2012098048A1 PROCESS FOR THE PREPARATION OF DIOL SULFONES 审中-公开
标题翻译：制备二氧化硅的方法
公开(公告)号：WO2012098048A1
公开(公告)日：2012-07-26
申请号：PCT/EP2012/050468
申请日：2012-01-13
申请人： DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V. , DE LANGE, Ben , RIEBEL, Peter, Hans , WOLBERG, Michael , HEEMSKERK, Dennis , MINK, Daniel
发明人： DE LANGE, Ben , RIEBEL, Peter, Hans , WOLBERG, Michael , HEEMSKERK, Dennis , MINK, Daniel
IPC分类号： C07D413/12 , C07D419/12
CPC分类号： C07D417/12 , C07D405/12 , C07D413/12 , C07D419/12
摘要： The present invention relates to a process for the preparation of a diol sulfone derivative comprising reaction of a halomethyl substrate with a thio-aryl compound to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.
摘要翻译：本发明涉及一种制备二醇砜衍生物的方法，包括卤甲基底物与硫代 - 芳基化合物的反应，得到硫醚化合物，并将硫代醚化合物氧化为相应的砜。在手性卤代甲基底物的情况下，所得手性二醇砜衍生物适合作为他汀类化合物的结构单元。

8. 发明申请

WO2007118682A1 PROCESS FOR THE PREPARATION OF ENANTIOMERI CALLY ENRICHED BETA-AMINO ALCOHOLS STARTING FROM GLYCINE AND AN ALDEHYDE IN THE PRESENCE OF A THREONINE ALDOLASE AND A DECARBOXYLASE 审中-公开
标题翻译：制备在丙二醛和十二烷基硫酸钠存在下从甘氨酸和阿尔德星开始的高效液相色谱法制备精氨酸的氨基酸醇的方法
公开(公告)号：WO2007118682A1
公开(公告)日：2007-10-25
申请号：PCT/EP2007/003274
申请日：2007-04-12
申请人： DSM IP ASSETS B.V. , SCHÜRMANN, Martin , MINK, Daniel , WOLBERG, Michael
发明人： SCHÜRMANN, Martin , MINK, Daniel , WOLBERG, Michael
IPC分类号： C12P13/00 , C12P13/06 , C12P41/00
CPC分类号： C12P13/001
摘要： The invention relates to a process for the preparation of an enantiomerically enriched β-amino alcohol, wherein glycine or a glycine salt and an aldehyde are reacted in the presence of a threonine aldolase and a decarboxylase to form the corresponding enantiomerically enriched β-aminoalcohol, and wherein at least either the threonine aldolase or the decarboxylase is β-selective. In a preferred embodiment of the invention at least either the threonine aldolase or the decarboxylase is enantioselective.
摘要翻译：本发明涉及制备对映体富集的β-氨基醇的方法，其中甘氨酸或甘氨酸盐和醛在苏氨酸醛缩酶和脱羧酶的存在下反应以形成相应的对映体富集的β-氨基醇，以及其中至少苏氨酸醛缩酶或脱羧酶是β选择性的。在本发明的优选实施方案中，苏氨酸醛缩酶或脱羧酶中的至少一种是对映选择性的。

9. 发明申请

WO2007068498A1 PROCESS FOR THE PREPARATION OF DELTA LACTONES 审中-公开
标题翻译：制备三角法的过程
公开(公告)号：WO2007068498A1
公开(公告)日：2007-06-21
申请号：PCT/EP2006/012141
申请日：2006-12-15
申请人： DSM IP ASSETS B.V. , MINK, Daniel , WOLBERG, Michael , SCHÜRMANN, Martin , HILKER, Iris
发明人： MINK, Daniel , WOLBERG, Michael , SCHÜRMANN, Martin , HILKER, Iris
IPC分类号： C12P17/06
CPC分类号： C12P17/06 , C07B53/00 , C07D309/10 , C07D309/30
摘要： The invention relates to a process for the preparation of δ-lactones by reacting acetaldehyde and a substituted acetaldehyde in the presence of an aldolase, preferably a DERA from Escherichia coli, from Bacillus subtilis or from a Geobacillus species, δ-lactones, such as saturated δ-lactones, α, β-unsaturated δ-lactones and 3-hydroxy- δ-lactones can suitably be used as (intermediates in the production of) flavors and/or fragrances and/or pharmaceuticals.
摘要翻译：本发明涉及通过乙醛和取代的乙醛在醛缩酶，优选来自大肠杆菌的DERA，来自枯草芽孢杆菌或地芽孢杆菌属物种，d-内酯如饱和食物的存在下反应来制备D-内酯的方法 D-内酯，α，β-不饱和的D-内酯和3-羟基-D-内酯可以适当地用作香料和/或香料和/或药物的（生产中的中间体）。

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