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1.发明授权
公开(公告)号：US5010012A
公开(公告)日：1991-04-23
申请号：US231290
申请日：1988-08-12
CPC分类号： C12P41/005 , A01N57/20 , C07F9/301 , C07F9/3211 , C12P9/00
摘要： Resolution of the racemates of phosphorus-containing functional acetic acid derivatives can be carried out in high yield and in enantiomeric purity using hydrolases such as esterases and lipases.
摘要翻译： 含磷官能乙酸衍生物的外消旋物的拆分可以使用水解酶如酯酶和脂肪酶以高产率和对映体纯度进行。
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公开(公告)号：US5496930A
公开(公告)日：1996-03-05
申请号：US315500
申请日：1994-09-30
申请人： Wolfgang Holla , Reinhold Keller
发明人： Wolfgang Holla , Reinhold Keller
IPC分类号： C07D309/30 , C12P17/06 , C07H1/00 , C07H5/04 , C07H5/06
CPC分类号： C07D309/30 , C12P17/06 , Y10S435/921
摘要： A process for highly regioselective esterification and ester cleavage on unsaturated sugar compounds with the aid of lipases and esterases, and products which can be prepared by this process.Highly regioselective esterifications and ester cleavages can be carried out on unsaturated sugar compounds with the aid of lipases and esterases. Lipases from microorganisms or from the pancreas and liver of animals are preferably used.
摘要翻译： 借助于脂肪酶和酯酶的不饱和糖化合物的高度区域选择性酯化和酯裂解的方法，以及可以通过该方法制备的产物。 借助于脂肪酶和酯酶，可以在不饱和糖化合物上进行高度区域选择性酯化和酯裂解。 优选使用来自微生物或来自动物的胰脏和肝脏的脂肪酶。
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3.发明授权Method for the enzymatic racemate resolution of racemic alcohols with/in vinyl esters by transesterification 失效通过酯交换反应用乙烯基酯消除外消旋醇的酶消旋物的方法
公开(公告)号：US4963492A
公开(公告)日：1990-10-16
申请号：US287371
申请日：1988-12-21
申请人： Reinhold Keller , Wolfgang Holla , Gerd Fulling
发明人： Reinhold Keller , Wolfgang Holla , Gerd Fulling
IPC分类号： A61K31/045 , C12P7/62 , C12P41/00
CPC分类号： C12P7/62 , C12P41/004
摘要： Racemic alcohols can be resolved in good yield and with high enantiomeric purity in the presence of vinyl esters with the aid of lipases from pig pancreas, pig liver and microorganisms.
摘要翻译： 借助于来自猪胰脏，猪肝和微生物的脂肪酶，外消旋醇可以以良好的产率和在乙烯基酯存在下具有高对映体纯度来解析。
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4.发明授权Process for highly regioselective esterification and ester cleavage on unsaturated sugar compounds with the aid of lipases and esterases 失效借助脂肪酶和酯酶对不饱和糖化合物进行高度区域选择性酯化和酯裂解的方法
公开(公告)号：US5380659A
公开(公告)日：1995-01-10
申请号：US924799
申请日：1992-08-06
申请人： Wolfgang Holla , Reinhold Keller
发明人： Wolfgang Holla , Reinhold Keller
CPC分类号： C07D309/30 , C12P17/06 , Y10S435/921
摘要： A process for highly regioselective esterification and ester cleavage on unsaturated sugar compounds with the aid of lipases and esterases, and products which can be prepared by this process.Highly regioselective esterifications and ester cleavages can be carried out on unsaturated sugar compounds with the aid of lipases and esterases. Lipases from microorganisms or from the pancreas and liver of animals are preferably used.
摘要翻译： 借助于脂肪酶和酯酶的不饱和糖化合物的高度区域选择性酯化和酯裂解的方法，以及可以通过该方法制备的产物。 借助于脂肪酶和酯酶，可以在不饱和糖化合物上进行高度区域选择性酯化和酯裂解。 优选使用来自微生物或来自动物的胰脏和肝脏的脂肪酶。
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公开(公告)号：US07803950B2
公开(公告)日：2010-09-28
申请号：US11676721
申请日：2007-02-20
申请人： Christophe Salagnad , Frank Zocher , Andreas Burgard , Bernd Junker , Rolf Hoerlein , Thomas Stuedemann , Claus-Jügen Maier , Jochen Hachtel , Wolfgang Holla , Christoph Tappertzhofen , Berndt Kulitzscher , Stephane Mutti
发明人： Christophe Salagnad , Frank Zocher , Andreas Burgard , Bernd Junker , Rolf Hoerlein , Thomas Stuedemann , Claus-Jügen Maier , Jochen Hachtel , Wolfgang Holla , Christoph Tappertzhofen , Berndt Kulitzscher , Stephane Mutti
IPC分类号： C07D263/32 , C12P7/62
CPC分类号： C07D413/12 , C07D263/62 , C07D309/12 , C12P17/14 , Y02P20/55
摘要： The invention relates generally to a process for preparing diarylcycloalkyl derivatives of the formula (I). wherein the respective R-group substituents are defined herein. These compounds of formula (I) are activators for peroxisome proliferator-activated receptors (PPAR activators) which are useful in the therapeutic treatment of a number of diseases and disorders of the central nervous system such as multiple sclerosis, Parkinson's Disease, psychiatric disorders and the like. The present invention is a novel process for preparing PPAR activators of the formula (I) which do not have the disadvantages of the processes known in the prior art. In particular, a process is provided with which the PPAR activators of formula (I) can be prepared in a suitable enantiomeric excess, i.e. high enantioselectivity, without the need for subsequent chiral chromatography.
摘要翻译： 本发明一般涉及式（I）的二芳基环烷基衍生物的制备方法。 其中相应的R基取代基在本文中定义。 这些式（I）化合物是过氧化物酶体增殖物激活受体（PPAR活化剂）的活化剂，其可用于治疗多种中枢神经系统的疾病和病症如帕金森病，帕金森病，精神障碍和 喜欢。 本发明是制备式（I）的PPAR活化剂的新方法，其不具有现有技术中已知方法的缺点。 特别地，提供了一种方法，其中式（I）的PPAR活化剂可以以合适的对映异构体过量即高对映选择性制备，而不需要随后的手性色谱法。
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公开(公告)号：US5262312A
公开(公告)日：1993-11-16
申请号：US689480
申请日：1991-04-23
申请人： Wolfgang Holla , Manfred Schudok
发明人： Wolfgang Holla , Manfred Schudok
IPC分类号： C07B61/00 , C07H15/04 , C07H15/10 , C07H15/18 , C07K9/00 , C12N9/24 , C12P17/06 , C12P19/44 , C12R1/19 , C12P19/04
摘要： It has been possible to show for a first time with the process according to the invention that the synthesis of glyco conjugates is possible by direct linkage of sugars with serine, serine derivatives and serine peptides with the aid of glucosidases.
摘要翻译： 可以通过本发明的方法第一次显示，糖链共轭物的合成可以通过糖与葡糖苷酶的丝氨酸，丝氨酸衍生物和丝氨酸肽的直接连接来实现。
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7.发明申请METHOD FOR THE PREPARATION OF ENANTIOMER FORMS OF CIS-CONFIGURED 3-HYDROXYCYCLOHEXANE CARBOXYLIC ACID DERIVATIVES USING HYDROLASES 审中-公开使用水解制备CIS配置的3-羟基环己烷羧酸衍生物的成膜剂形式的方法公开(公告)号：US20070197788A1
公开(公告)日：2007-08-23
申请号：US11669545
申请日：2007-01-31
IPC分类号： C07F7/02 , C07D413/02 , C07D263/02
CPC分类号： C12P41/004 , C12P7/00 , C12P17/00
摘要： The present invention relates to a process for preparing chiral non-racemic cis-configured cyclohexanols or cyclohexanol derivatives of the formula (I) Cis-configured hydroxyl-cyclohexane carboxylic acid derivatives of formula (I) are central building blocks or immediate precursors for the medicinally active compounds which allow a therapeutic modulation of the lipid and/or carbohydrate metabolism and are thus suitable for preventing and/or treating type II diabetes, hyperglycemia and artherosclerosis. The cis-configured hydroxyl-cyclohexane carboxylic acid derivatives of formula (I) are central building blocks or immediate precursors for the medicinally active compounds described in the prior art.
摘要翻译： 本发明涉及制备式（I）的手性非外消旋顺式配位的环己醇或环己醇衍生物的方法。式（I）的顺式构型的羟基 - 环己烷羧酸衍生物是用于药物的中心结构单元或直接前体 允许治疗性调节脂质和/或碳水化合物代谢并因此适合于预防和/或治疗II型糖尿病，高血糖症和动脉粥样硬化的活性化合物。 式（I）的顺式构型的羟基 - 环己烷羧酸衍生物是现有技术中描述的药物活性化合物的中心构建块或立即前体。
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8.发明授权公开(公告)号：US09340489B2
公开(公告)日：2016-05-17
申请号：US14118705
申请日：2012-05-21
申请人： Jens Atzrodt , Volker Derdau , Wolfgang Holla , Matthias Beller , Lorenz Neubert , Dirk Michalik
发明人： Jens Atzrodt , Volker Derdau , Wolfgang Holla , Matthias Beller , Lorenz Neubert , Dirk Michalik
IPC分类号： C07C217/28 , C07B59/00 , C07C211/07 , C07C211/08 , C07C211/27 , C07D207/06 , C07D211/14 , C07D223/04 , C07D241/04 , C07D401/04
CPC分类号： C07C217/28 , C07B59/00 , C07C211/07 , C07C211/08 , C07C211/27 , C07D207/06 , C07D211/14 , C07D223/04 , C07D241/04 , C07D401/04
摘要： The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.
摘要翻译： 本发明涉及通过使用氘源和基于钌（II）的催化剂，在N-原子的α和/或β位上氘化胺的方法。
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9.发明授权Method for the production of oxazoles by condensing aromatic aldehydes with α-ketoximes to N-oxides and then reacting the same with activated acid derivatives 有权通过将芳香族醛与α-酮肟缩合成N-氧化物然后使其与活性酸衍生物反应生产恶唑的方法公开(公告)号：US07825144B2
公开(公告)日：2010-11-02
申请号：US12509853
申请日：2009-07-27
申请人： Wolfgang Holla , Rolf-Ludwig Hoerlein , Berndt Kulitzscher , Wolfgang Laux , Thomas Stuedemann , Christoph Tappertzhofen , Robert J. H. Scheffer
发明人： Wolfgang Holla , Rolf-Ludwig Hoerlein , Berndt Kulitzscher , Wolfgang Laux , Thomas Stuedemann , Christoph Tappertzhofen , Robert J. H. Scheffer
IPC分类号： A61K31/421 , C07D263/30
CPC分类号： C07D263/32
摘要： The invention is related to a process for preparing compounds of the formula IV by means of conversion of aromatic aldehydes of the formula I using α-ketoximes of the formula II via N-oxides of the formula III to halomethyloxazoles of the formula IV, wherein R1, R2, R3, R4, R5, R6, R7, R8, X1, X2, X3, o, n1 and n2 are as defined herein.
摘要翻译： 本发明涉及一种制备式Ⅳ化合物的方法，该方法是通过使式Ⅶ的α-酮肟通过式III的N-氧化物转化为式Ⅳ的卤代甲氧基，将式Ⅰ的芳族醛转化成式Ⅳ的卤代甲氧基唑，其中R 1 ，R2，R3，R4，R5，R6，R7，R8，X1，X2，X3，o，n1和n2如本文所定义。
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10.发明授权公开(公告)号：US06407258B1
公开(公告)日：2002-06-18
申请号：US09601032
申请日：2000-07-26
IPC分类号： C07D23390
CPC分类号： C07D233/90
摘要： The invention relates to a process for the preparation of compounds of the formula (I) in which R(2) and R(3) independently of one another are —SR(4) or —COOR(5) and R(1), R(4) and R(5) have the meaning indicated in the description, which comprises cyclizing compounds of the formula II in which R(1), R(2) and R(3) have the meaning defined above, in the presence of alkylphosphonic anhydrides to give compounds of the formula (I), then purifying these in as is known per se by salt formation and, if appropriate, subsequent recrystallization and optionally removing radicals introduced for the protection of other functional groups in a manner known per se; and their use as intermediate for the synthesis of active compounds.
摘要翻译： 本发明涉及制备式（I）化合物的方法，其中R（2）和R（3）彼此独立地为-SR（4）或-COOR（5）和R（1）， R（4）和R（5）具有说明书中指出的含义，其包括使R（1），R（2）和R（3）具有上述定义的式IIin的环化化合物在 烷基膦酸酐，得到式（I）化合物，然后如本身已知的那样通过盐形成和如果合适的话进行随后的重结晶和任选地除去引入的保护其它官能团的基团以本身已知的方式纯化; 以及它们作为合成活性化合物的中间体的用途。
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