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1. 发明申请

US20150175527A1 SYNTHESIS OF DIAMIDO GELLANTS BY USING AMINO ACID N-CARBOXYANHYDRIDES 有权
标题翻译：使用氨基酸N-羧酸的DIAMIDO GELLANTS的合成
公开(公告)号：US20150175527A1
公开(公告)日：2015-06-25
申请号：US14402847
申请日：2013-05-13
申请人： Martin Bindl , Roland Herrmann , Gunter Knaup
发明人： Martin Bindl , Roland Herrmann , Gunter Knaup
IPC分类号： C07C231/02
CPC分类号： C07C231/02 , C07C2601/14 , C07D263/44 , C07C237/20 , C07C237/10
摘要： The invention relates to a method for the synthesis of a compound according to formula I comprising the following steps: a) reacting a N-carboxyanhydride according to formula II and a N-carboxy-anhydride according to formula III with a diamine according to formula IV and b) adding an acid to the reaction to adjust the pH value of the reaction to
摘要翻译：本发明涉及一种合成式I化合物的方法，包括以下步骤：a）使根据式II的N-羧酸酐和根据式III的N-羧酸酐与根据式IV的二胺反应和b）向反应物中加入酸以将反应的pH值调节至<7; 其中L表示C2-C20烷基，C6-C20芳基或C7-C20烷基芳基; R1和R2可以相同或不同，表示氢原子，C1-C4烷基，C1-C4羟烷基，C1-C4硫醚基，C6-C20芳基，C7-C20烷基芳基， C 7 -C 20烷基羟基芳基，具有1至4个杂原子的C 4 -C 20烷基杂芳基; 或可以是酸，酰胺或可以被C 1 -C 6烷基或C 7 -C 20烷基芳基酯化的C 1 -C 4烷基羧酸部分。

2. 发明授权

US5731459A Process for separating amino acids and aminosulponic acids through adsorption on zeolites 失效
标题翻译：通过吸附沸石分离氨基酸和氨基磺酸的方法
公开(公告)号：US5731459A
公开(公告)日：1998-03-24
申请号：US704976
申请日：1996-08-28
申请人： Stefan Stockhammer , Wiltrud Schafer-Treffenfeldt , Gunter Knaup , Karlheinz Drauz , Elfriede Sextl
发明人： Stefan Stockhammer , Wiltrud Schafer-Treffenfeldt , Gunter Knaup , Karlheinz Drauz , Elfriede Sextl
IPC分类号： C07D207/16 , B01J20/18 , C07B63/00 , C07C209/86 , C07C227/40 , C07C229/08 , C07C229/24 , C07C229/26 , C07C229/36 , C07C231/24 , C07C233/47 , C07C279/14 , C07C303/44 , C07K1/14 , C07K5/06 , C07C51/48 , C07C51/487 , C07C227/28
CPC分类号： C07C227/40
摘要： The invention relates to a process for removing amino acids and/or aminosulphonic acids from preferably aqueous solutions which contain these as impurities by adsorbing the amino acids on zeolites. Solutions to which the process according to the invention can be applied are produced, for example, from the industrial synthesis of oligopeptides in which the amino acids serving as starting materials are always present in solution, sometimes to a not inconsiderable residual concentration, together with the desired end product.
摘要翻译：本发明涉及从优选含有这些杂质的水溶液中除去氨基酸和/或氨基磺酸的方法，该方法通过将氨基酸吸附在沸石上。根据本发明的方法可以应用的溶液例如由工业上合成的寡肽制成，其中作为起始原料的氨基酸总是存在于溶液中，有时甚至不可忽略的残留浓度，以及期望的最终产品。

3. 发明授权

US6156908A Procedure for the manufacture of 3-amino-2-oxo-pyrrolidines, new intermediates and their use 有权
标题翻译：制备3-氨基-2-氧代吡咯烷酮，新中间体及其用途的方法
公开(公告)号：US6156908A
公开(公告)日：2000-12-05
申请号：US393874
申请日：1999-09-10
申请人： Karlheinz Drauz , Ingo Klement , Gunter Knaup
发明人： Karlheinz Drauz , Ingo Klement , Gunter Knaup
IPC分类号： C07C323/60 , C07C381/12 , C07D207/26 , C07D207/273 , C07D207/40 , C07D315/00 , C07D321/00
CPC分类号： C07D207/273 , C07C381/12 , Y02P20/55
摘要： The invention is directed to a process for the preparation of lactams of Formula I. It is further directed to new advantageous intermediates of Formula II and the use thereof. By the cyclization of compounds of Formula II, compounds of Formula I are obtained.
摘要翻译：本发明涉及制备式I的内酰胺的方法。还涉及式II的新的有利的中间体及其用途。通过式II化合物的环化，得到式I化合物。

4. 发明授权

US6114163A Process for obtaining active L-.alpha.-amino carboxylic acids from corresponding racemic d, L-.alpha.-amino carboxylic acids 失效
标题翻译：从相应的外消旋d，L-α-氨基羧酸获得活性的L-α-氨基羧酸的方法
公开(公告)号：US6114163A
公开(公告)日：2000-09-05
申请号：US94321
申请日：1998-06-16
申请人： Karlheinz Drauz , Andreas Bommarius , Michael Karrenbauer , Gunter Knaup
发明人： Karlheinz Drauz , Andreas Bommarius , Michael Karrenbauer , Gunter Knaup
IPC分类号： C07C227/34 , C07C227/36 , C07C319/20 , C07C323/60 , C12P13/04 , C12P41/00 , C07C1/00
CPC分类号： C12P41/007 , C07C227/34 , C07C227/36 , C07C319/20 , C12P13/04
摘要： The disclosure relates to a process for obtaining optically active L-.alpha.-aminocarboxylic acids from the corresponding racemic D,L,.alpha.-aminocarboxylic acids. The following steps are involved: (a) the D,L,.alpha.-aminocarboxylic acids are acetylated; (b) the N-acetyl-L-.alpha.-aminocarboxylic acid present in the mixture of N-acetyl-D,L,.alpha.-aminocarboxylic acids thus obtained is broken down enzymatically into the L-.alpha.-aminocarboxylic acid; (c) the L-.alpha.-aminocarboxylic acid is separated from the mixture, a quantity of a solution of N-acetyl-D(L)-.alpha.-aminocarboxylic acids and a quantity of acetate equivalent to the L-.alpha.-aminocarboxylic acid being retained; and (d) the N-acetyl-D(L)-.alpha.-aminocarboxylic acid is racemized and recycled for enzymatic breakdown. Known extraction processes involving steps (a) to (d) have the disadvantage of producing large quantities of salt. Specifically, the processes are far removed from the ideal equation, according to which one hundred percent of the acetic anhydride and the D,L,.alpha.-aminocarboxylic acids are converted to L-.alpha.-aminocarboxylic acids and acetic acid. Adjusting the retained solution from step (c) in such a way as to obtain a solution consisting essentially of N-acetyl-D-(L)-.alpha.-aminocarboxylic acid salt and free acetic acid in equilibrium with acetate and free N-acetyl-D(L)-.alpha.-aminocarboxylic acid and from which acetic acid is extracted by distillation makes it surprisingly easy to feed the solution formed as "mother liquor" following separation of the L-.alpha.-aminocarboxylic acid in the circuit and to achieve a materials balance as close as possible to the ideal.
摘要翻译：本公开涉及从相应的外消旋D，L，α-氨基羧酸获得光学活性的L-氨基羧酸的方法。涉及以下步骤：（a）D，L，α-氨基羧酸被乙酰化; （b）将由此获得的N-乙酰基-D，L，α-氨基羧酸的混合物中存在的N-乙酰基-L-α-氨基羧酸酶促分解成L-氨基羧酸; （c）从混合物中分离出L-α-氨基羧酸，一定量的N-乙酰基-D（L）-α-氨基羧酸溶液和一定量的乙酸钠相当于L-氨基羧酸为保留和（d）N-乙酰基-D（L）-α-氨基羧酸被外消旋化并再循环用于酶分解。涉及步骤（a）至（d）的已知提取方法具有产生大量盐的缺点。具体来说，这些方法远远不能从理想方程中去除，根据其中百分之百的乙酸酐和D，L，α-氨基羧酸被转化成L-α-氨基羧酸和乙酸。调节步骤（c）中保留的溶液，以获得基本上由N-乙酰基-D-（L）-α-氨基羧酸盐和游离乙酸与乙酸酯和游离N-乙酰基 - D（L）-α-氨基羧酸，通过蒸馏萃取乙酸，使得在电路中分离出L-α-氨基羧酸之后，使得形成为“母液”的溶液容易进料，并获得材料平衡尽可能接近理想。

5. 发明申请

US20080015368A1 Process for preparing beta-amino-alpha-hydroxycarboxamides 有权
标题翻译：制备β-氨基-α-羟基甲酰胺的方法
公开(公告)号：US20080015368A1
公开(公告)日：2008-01-17
申请号：US11819964
申请日：2007-06-29
申请人： Gunter Knaup
发明人： Gunter Knaup
IPC分类号： C07D301/00 , C07C233/06 , C07D303/38
CPC分类号： C07D303/48 , C07C231/12 , C07C231/20 , C07C237/04 , C07C271/22 , C07C2601/02
摘要： The present invention is directed to a process for preparing β-amino-α-hydroxycarboxamides. The process works with epoxycarboxamides of the formula 2 which are reacted with ammonia or other amines.
摘要翻译：本发明涉及一种制备β-氨基-α-羟基甲酰胺的方法。该方法与式2的环氧羧酰胺与氨或其它胺反应。

6. 发明授权

US06080887A Process for racemization of N-acetyl-(D)L-.alpha.-amino carboxylic acids 失效
标题翻译： N-乙酰基 - （D）L-α-氨基羧酸外消旋化的方法
公开(公告)号：US06080887A
公开(公告)日：2000-06-27
申请号：US95409
申请日：1998-06-10
申请人： Karlheinz Drauz , Michael Karrenbauer , Andreas Bommarius , Gunter Knaup
发明人： Karlheinz Drauz , Michael Karrenbauer , Andreas Bommarius , Gunter Knaup
IPC分类号： C07C231/16 , C07C233/47 , C07B55/00
CPC分类号： C07C231/16
摘要： With known methods of racemizing N-acetyl-D(L)-.alpha.-amino carboxylic acids in the non-aqueous state by heating them to temperatures above room temperatures, significant quantities of by-products are formed, especially acetyl dipeptides. By converting at least a proportion of the N-acetyl-D(L)-.alpha.-amino carboxylic acids to corresponding N-acetyl-D(L)-.alpha.-amino carboxylic acid salts before or during the heating, it is possible to increase the sojourn time of the educt which is to be racemized at higher temperatures without any evident increase in the quantity of by-product formed (in particular acetylated dipeptides). Also disclosed is the production of optically active amino acids by enzymatic splitting of racemic compounds.
摘要翻译：通过将N-乙酰基-D（L）-α-氨基羧酸在非水状态下外消旋加热到室温以上的已知方法，形成显着量的副产物，特别是乙酰二肽。通过在加热之前或期间将至少一部分N-乙酰基-D（L）-α-氨基羧酸转化为相应的N-乙酰基-D（L）-α-氨基羧酸盐，可以增加即将在更高的温度下外消旋的流出物的停留时间不会形成副产物（特别是乙酰化的二肽）的量的明显增加。还公开了通过外消旋化合物的酶裂解生产光学活性氨基酸。

7. 发明授权

US6051715A Method of producing oxazolidinones, the use thereof and novel oxazolidinones 失效
标题翻译：制备恶唑烷酮的方法，其用途和新的恶唑烷酮
公开(公告)号：US6051715A
公开(公告)日：2000-04-18
申请号：US894519
申请日：1997-08-21
申请人： Karlheinz Drauz , Gunter Knaup , Stefan Retzow
发明人： Karlheinz Drauz , Gunter Knaup , Stefan Retzow
IPC分类号： C07C231/14 , C07C237/22 , C07D263/18 , C07D263/04
CPC分类号： C07D263/18 , C07C231/14 , C07C237/22
摘要： The invention concerns a method of producing oxazolidinones of formula (I), wherein R.sup.1 -R.sup.5 have the meanings given in the description, by reacting cyclical anhydrides of formula (II) with carbonyl compounds of general formula (III) at temperatures between ambient temperature and approximately 150.degree. C. The invention also concerns the production of the cyclical anhydrides of formula (II) by reacting N-protected aminodicarboxylic acids of formula (IV) with a dehydrating agent in situ. The invention further concerns the use of oxazolidinones of formula (I) for the .alpha.-selective production of esters of formula (V) and amides of general formula (VII).
摘要翻译： PCT No.PCT / EP96 / 00390 Sec。 371日期1997年8月21日 102（e）日期1997年8月21日PCT提交1996年1月31日PCT公布。公开号WO96 / 26194 日期：1996年8月29日本发明涉及一种制备式（I）的恶唑烷酮的方法，其中R1-R5具有本说明书中给出的含义，通过使式（II）的环状酸酐与通式（III）的羰基化合物反应在环境温度和约150℃之间的温度。本发明还涉及通过将式（IV）的N-保护的氨基二羧酸与脱水剂原位反应来生产式（II）的环状酸酐。本发明还涉及式（I）的恶唑烷酮用于α-选择性生产式（V）的酯和通式（VII）的酰胺的用途。

8. 发明授权

US5874121A Method of producing L-aspartyl-D-alanine-N-(thiethane-3-yl)-amides 失效
标题翻译： L-天冬氨酰-D-丙氨酸-N-（硫醚-3-基） - 酰胺的制备方法
公开(公告)号：US5874121A
公开(公告)日：1999-02-23
申请号：US894518
申请日：1997-11-21
申请人： Karlheinz Drauz , Gunter Knaup , Stefan Retzow , Michael Schwarm , Christoph Weckbecker
发明人： Karlheinz Drauz , Gunter Knaup , Stefan Retzow , Michael Schwarm , Christoph Weckbecker
IPC分类号： C07K5/072 , C07K5/075 , C07D103/52 , C07D307/22 , C07C87/34 , C07D103/50
CPC分类号： C07K5/06113 , Y02P20/55
摘要： The invention concerns a method of producing L-aspartyl-D-alanine-N-(thietane-3-yl) amides of general formula I by reacting D-alanine-thietane amides of general formula II with oxazolidinone compounds of general formula III in an inert organic solvent, wherein R.sup.1 stands for H or a selectively separable protective group, R.sup.2 -R.sup.5 independently of one another, are identical or different and stand for H or linear or branched C.sub.1 -C.sub.4 -alkyl, and R.sup.6 and R.sup.7, independently of each other, are identical or different and stand for H, linear or branched C.sub.1 -C.sub.4 -alkyl, aryl or a group which activates the carbonyl group. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 00393 Sec。 371日期：1997年11月21日 102（e）1997年11月21日PCT PCT 1996年1月31日PCT公布。出版物WO96 / 26213 PCT 日期：1996年8月29日本发明涉及通式I的D-丙氨酸 - 硫杂环丁烷酰胺与通式II的D-丙氨酸 - 硫杂环丁烷酰胺与恶唑烷酮化合物的反应生产L-天冬氨酰-D-丙氨酸-N-（硫杂环丁烷-3-基）通式III在惰性有机溶剂中，其中R1代表H或选择性可分离的保护基，R2-R5彼此独立地相同或不同，代表H或直链或支链C1-C4烷基，R6和 R 7彼此独立地相同或不同，代表H，直链或支链C 1 -C 4 - 烷基，芳基或活化羰基的基团。（一）图像（二）<图像>（三）

9. 发明授权

US5534538A N-acyl dipeptides and their compositions 失效
标题翻译： N-酰基二肽及其组成
公开(公告)号：US5534538A
公开(公告)日：1996-07-09
申请号：US194568
申请日：1994-02-10
申请人： Karlheinz Drauz , Gunter Knaup , Ulrich Groeger
发明人： Karlheinz Drauz , Gunter Knaup , Ulrich Groeger
IPC分类号： A61K38/00 , A23L33/17 , C07K5/06 , C07C233/00 , A61K31/16 , A61K31/405 , A61K31/415 , C07C233/24 , C07C233/34
CPC分类号： C07K5/06043 , A23L33/17 , C07K5/06026 , A61K38/00
摘要： Novel a-acyl dipeptides of the formula:R.sup.2 --NH--CHR.sup.1 --O--ASin which AS, R.sup.1 and R.sup.2 have certain, more precisely defined meanings. These N-acyl dipeptides are more stable under conditions of sterilization (121.degree. C.) than corresponding, non-acylated dipeptides. On the other hand, they are cleaved more rapidly and more completely at the peptide bond in the living organism than the cleavage of the acyl group from simple N-acyl amino acids takes place. They can therefore be used with advantage as a source for the carbon terminal amino acid in mixtures and solutions for artificial nutrition or in culture media for cell cultures.
摘要翻译：新型α-酰基二肽，其分子式为：R2-NH-CHR1-O-AS，其中AS，R1和R2具有一定的更精确定义的含义。这些N-酰基二肽在灭菌（121℃）条件下比相应的非酰化二肽更稳定。另一方面，它们在活体中的肽键处比从简单的N-酰基氨基酸裂解酰基更快速和更完全地裂解。因此，它们可以有利地用作人造营养物质或培养基中混合物和溶液中碳末端氨基酸的来源。

10. 发明授权

US5116872A Microbicidal compositions 失效
标题翻译：微生物组合物
公开(公告)号：US5116872A
公开(公告)日：1992-05-26
申请号：US643882
申请日：1991-01-22
申请人： Peter Ackermann , Hanspeter Fischer , Rolf Vogel , Karlheinz Drauz , Hans-Albrecht Hasseberg , Hans-Jochen Hasselbach , Gunter Knaup , Hans-Peter Krimmer , Matthias Schafer
发明人： Peter Ackermann , Hanspeter Fischer , Rolf Vogel , Karlheinz Drauz , Hans-Albrecht Hasseberg , Hans-Jochen Hasselbach , Gunter Knaup , Hans-Peter Krimmer , Matthias Schafer
IPC分类号： A01N37/44 , C07C229/48 , C07C229/76
CPC分类号： C07C229/76 , A01N37/44 , C07C229/48 , C07C2101/14
摘要： 1-Aminocyclohexanecarboxylic acid derivatives of the formula I ##STR1## or their acid addition salts or a metal complex can be employed for protecting plants from microorganisms. In the formula I, R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl, or an ammonium radical which is unsubstituted or substituted by hydrocarbon radicals having not more than 20 C atoms, or a metal ion equivalent.Compounds of the formula I can be employed in the form of crop protection agents using suitable carrier materials.
摘要翻译：式I（I）的1-氨基环己烷羧酸衍生物或其酸加成盐或金属络合物可用于保护植物免受微生物侵害。在式I中，R 1是氢或C 1 -C 4烷基，R 2是氢，C 1 -C 6烷基，苄基或未被取代或被不大于20个碳原子的烃基取代的铵基或金属离子当量。式I的化合物可以使用合适的载体材料以作物保护剂的形式使用。

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