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1. 发明申请

WO1995030740A1 PROCESS FOR OBTAINING MICRO-ORGANISMS CONTAINING PEPTIDE AMIDASE, MICRO-ORGANISMS OBTAINED THEREWITH, PEPTIDE AMIDASES CONTAINED IN THEM AND USE THEREOF 审中-公开
标题翻译：一种获得肽含微生物使得WON微生物，THEREIN肽酰胺酶及其用途
公开(公告)号：WO1995030740A1
公开(公告)日：1995-11-16
申请号：PCT/EP1995001689
申请日：1995-04-29
申请人： DEGUSSA AKTIENGESELLSCHAFT , STELKES-RITTER, Ursula , KULA, Maria-Regina , WYZGOL, Klaudia , BOMMARIUS, Andreas , SCHWARM, Michael , DRAUZ, Karlheinz
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C12N01/20
CPC分类号： C12R1/64 , C12N9/80
摘要： A plant peptide amidase from the flavedo of oranges is known; this can be obtained only in small quantities and is seasonal. The proposed new enzymes are microbial peptide amidases which can be obtained from micro-organisms recovered from soil samples in a "double screening" and grown. These microbial peptide amidases are particularly useful for (a) the production of peptides and N-terminal-protected amino acids, (b) racemate splitting of N-protected amino acid amides, (c) obtaining non-proteinogenous D-amino acids, and (d) obtaining new N alpha -protected D-amino acid amides.
摘要翻译：已知的植物的肽从橙汁的flavedo。这只能小批量和季节性拿下。新的酶是微生物肽酰胺酶，其可从在一“双筛选”从土壤样品得到的和繁殖微生物。微生物肽酰胺酶是特别有用的）肽和N-末端保护的氨基酸，b）决议的N-保护的氨基酸酰胺的制备，c）回收nonproteinogenic D-氨基酸，d）获得新的N-阿尔法 - 保护的D-氨基酸酰胺。

2. 发明申请

WO1997021667A1 PROCESS FOR THE PRODUCTION OF N-ACETYL-D,L-ALPHA-AMINOCARBOXYLIC ACIDS 审中-公开
标题翻译：用于生产N-乙酰基-D，L-α-氨基羧酸
公开(公告)号：WO1997021667A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005439
申请日：1996-12-05
申请人： DEGUSSA AKTIENGESELLSCHAFT , DRAUZ, Karlheinz , BOMMARIUS, Andreas , KARRENBAUER, Michael , KNAUP, Günter
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07C231/02
CPC分类号： C07C319/28 , C07C231/02 , C07C233/47 , C07C319/20 , C12P41/007 , C07C323/59
摘要： Known acetylation processes for producing N-acetyl-D,L- alpha -aminocarboxylic acids from the corresponding D,L- alpha -aminocarboxylic acids by acetylation with acetic anhydride in acetic acid and isolation of the resulting N-acetyl-D,L- alpha -aminocarboxylic acids from the acetylation mixture either result in the production of large quantities of salts or require an aqueous treatment to isolate the N-acetylated alpha -amino acids in sufficiently pure form. By carrying out the acetylation at 60-150 DEG C in a concentration of
摘要翻译：在已知的乙酰化用于制备N-乙酰基-D，L--α-氨基从相应的D氨基酸，L-α-氨基羧酸的乙酰化与在乙酸和所得到的N-乙酰基-D-的隔离，L-α-氨基从氨基酸乙酸酐或者乙酰化产生不可避免生产高量的盐，或它是必要的N-乙酰化的α-氨基酸在足够纯度的回收的含水制剂。在60中，所述乙酰化，其特征在于，以150℃下在<3摩尔每1升乙酸的α-氨基羧酸的方法，其中获得关于压力和温度标准条件的浓度的浓度的N-乙酰基-D，L-执行，并且的α-氨基羧酸通过蒸发作为熔体或固体得到，可以用含水制剂被完全分配，同时仍然非常高的品质都在产率和纯度方面得以实现。 N-乙酰-D，L-α-氨基羧酸为在方法的酶裂解为使用制备光学活性的α-氨基羧酸。

3. 发明申请

WO1997021663A1 PROCESS FOR OBTAINING OPTICALLY ACTIVE L-ALPHA-AMINOCARBOXYLIC ACIDS FROM CORRESPONDING RACEMIC D,L-ALPHA-AMINOCARBOXYLIC ACIDS 审中-公开
标题翻译： PROCEDURE用于获得光学活性的L-α-氨基酸羧酸OFF相应的外消旋D，L-α-氨基羧酸
公开(公告)号：WO1997021663A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005440
申请日：1996-12-05
申请人： DEGUSSA AKTIENGESELLSCHAFT , DRAUZ, Karlheinz , BOMMARIUS, Andreas , KARRENBAUER, Michael , KNAUP, Günter
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07C227/34
CPC分类号： C12P13/04 , C07C227/34 , C07C227/36 , C07C319/20 , C12P41/007 , C07C323/60
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 with 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 racemised and recycled for enzymatic breakdown. Known extraction processes involving steps (a) to (d) have the disadvantage of producing large quantities of salts. 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 acids in the circuit and to achieve a materials balance as close as possible to the ideal.
摘要翻译：公开了一种用于从相应的外消旋D，L-α氨基羧酸中，D，L-α-氨基羧酸获得的光学活性的L-α-氨基酸的方法被乙酰化，其中（a）; （B）的氨基羧酸在这样获得的N-乙酰基D的混合物，L-α本N-乙酰基-L-阿尔法氨基羧酸酶促到的L-α-氨基羧酸切割; （C）所述的L-α-氨基羧酸从混合物的回退的N-乙酰基-D-（L）下分离 - α氨基羧酸和含乙酸溶液的L-形成α氨基羧酸等价量的一种; 和溶液中所含的N-乙酰基-D-（L）（D） - 是α-氨基羧酸外消旋化和再循环的酶促切割。在已知的回收方法，其中所述步骤（a）至（d），大量盐负荷降低到不利的。特别地，理想的方程的方法，在这之后的乙酸酐和D，L-α-氨基羧酸是百分之百的L-α-氨基羧酸和乙酸，远。特征在于，所述返回保留从步骤（c）的溶液被调整，使得基本上正式N-乙酰基D（L） - α-aminocarbonsäuresalz和游离乙酸平衡用乙酸和游离N-乙酰基-D-（L） - 得到的α-氨基羧酸现有的解决方案，从其中通过蒸馏除去乙酸，有可能以一种非常简单的方式，导致使用该电路的L-α-氨基羧酸为“母液”和理想的一个尽可能靠近物料平衡分离后的溶液供给实现。

4. 发明申请

WO1996001906A1 KINETICALLY CONTROLLED PROCESS FOR ENZYMATIC PRODUCTION OF PEPTIDES 审中-公开
标题翻译：动力学方法对于酶法生产肽
公开(公告)号：WO1996001906A1
公开(公告)日：1996-01-25
申请号：PCT/EP1995002655
申请日：1995-07-07
申请人： DEGUSSA AKTIENGESELLSCHAFT , JAKUBKE, Hans-Dieter , HÄNSLER, Marion , WALDMANN, Herbert , DRAUZ, Karlheinz , BOMMARIUS, Andreas
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C12P21/02
CPC分类号： C07K1/062 , C12P21/02 , Y02P20/55
摘要： The invention pertains to a kinetically controlled process for enzymatic production of fully protected peptides formula (III): X-NH-A -CO-NH-A -CO-Y, wherein fully protected amino acid esters of formula (I): X-NH-A -CO-Y' as acyl donor, in which X and Y' are protective groups and A is an amino acid or peptide radical, are reacted with Y-protected amino acids or peptides of formula (II): NH2-A -CO-Y (as nucleophiles), in which Y' is a different protective group and A is an amino acid or peptide radical, in the presence of a biocatalyst (e.g. protease, preferably chymotrypsin or trypsin or (choline)-esterase), characterized in that Y' is choline or one of its salts and that the biocatalyst is an enzyme that catalyzes the cleaving to the choline-ester bond and the transfer of the acyl radical X-NH-A -CO to the compound of formula (II). The choline estes lend solubility properties and efficient acyl-donor properties for the biocatalytic linkage of peptide bonds.
摘要翻译：本发明涉及控制一个kinetish，酶法生产式（III）的完全保护的肽的方法：NH-A <1> -CO-NH-A <2> -CO-Y，其中式vollgestüzte氨基酸巢（I）：X -NH-A <1> -CO-Y '作为酰基供体，其中X和Y' 保护基团，和一个<1>代表氨基酸或肽残基，Y保护的氨基酸或式的肽（II）：NH2-A < 2> CO-Y是（如亲核试剂），其中Y“是不同的保护基团，和一个<2>是氨基酸或肽残基，在生物催化剂的存在下（Z。B.蛋白酶，优选胰蛋白酶或胰凝乳蛋白酶或（胆碱）酯酶）Y 进行反应，其特征在于，Y“胆碱或它们的盐是指，并且所述生物催化剂是胆碱酯键的裂解和酰基X-NH-A <1>为-CO式的化合物的转移（II）被催化酶。胆碱传授的溶解性和有效的用于Acyldonoreigenschaftem生物催化的肽键形成。

5. 发明申请

WO1994008974A1 METHOD OF PREPARING AMINOALKYLHYDANTOINS AND AMINOALKYL-'alpha'-AMINOACIDS 审中-公开
标题翻译：工艺用于生产和AMINOALKYLHYDANTOIN氨基α-氨基酸
公开(公告)号：WO1994008974A1
公开(公告)日：1994-04-28
申请号：PCT/EP1993002753
申请日：1993-10-08
申请人： DEGUSSA AKTIENGESELLSCHAFT , KOTTENHAHN, Matthias , DRAUZ, Karlheinz , BOMMARIUS, Andreas
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07D233/76
CPC分类号： C07C227/24 , C07D233/76 , Y02P20/55
摘要： In order to prepare aminoalkylhydantoins, the amino function must be protected before the formation of the hydantoin ring. Since the protective group is difficult to remove again, however, in particular for subsequent enzymatic reactions in which the corresponding aminoacids are liberated, a simple method of preparing aminoalkyl compounds was sought. The invention calls for an acid-labile amino-protecting group to be used in the preparation of compounds of general formula (I) or (II) in which X is alkylene and Y is hydrogen or alkyl. This protective group can even be split off during the acid-catalysed hydantoin ring closure since, during this step, no competing reactions of the freed amino function take place. The method disclosed is suitable for use in the preparation of optically opposite D- and L-forms of natural and synthetic aminoacids.

6. 发明申请

WO1997029837A2 PROCESS FOR SEPARATING SUBSTANCES USING A SUITABLE MEMBRANE 审中-公开
标题翻译：方法用于分离物质通过适当的REED手段
公开(公告)号：WO1997029837A2
公开(公告)日：1997-08-21
申请号：PCT/EP1997000734
申请日：1997-02-17
申请人： DEGUSSA AKTIENGESELLSCHAFT , WANDREY, Christian , KRAGL, Udo , BOMMARIUS, Andreas , DRAUZ, Karlheinz
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： B01D61/02
CPC分类号： C07C51/42 , B01D61/02 , B01J4/04 , B01J19/2475
摘要： In catalytic reactions and reactions requiring synthesis-promoters, it is useful to be able to separate the promoter from the product formed and thus make it available for recycling. One possible way of achieving this separation is by immobilising the synthesis-promoter on special carriers. This, however, often reduces the contact area between the promoter and carrier and thus markedly reduces the reactivity of the promoter or alters its mode of action. The immobilisation process itself may also present problems in terms of working time spent and catalyst loss. If the product and promoter in a catalytic reaction are separated by filtration using a nanofiltration or reverse osmosis membrane, it is possible, even when the weight differences between promoter and product are relatively small and provided that the retension differences are sufficient and the associated recovery rate of the promoter therefore high, to dispense with separation based on immobilisation techniques. The process proposed can be used for separating reaction mixtures for catalytic reactions with the aim of efficiently producing organic synthesis products or optically active organic compounds.
摘要翻译：在催化反应中和在需要合成助剂反应中，有利的是能够以该辅助物质从所得产物中分离，从而使回收访问。单程为达到这个间距，合成佐剂特定运营商的固定。这通常，但在赋形剂和载体之间的接触面积减少，由此，辅助剂的反应性大大降低的或改变的佐剂的作用模式是要被记录。此外，劳动和催化剂损失方面的固定化过程中也不是没有问题。其特征在于，产品和赋形剂在催化反应通过纳的分离通过过滤或反渗透膜进行时，即使在佐剂和产品之间的佐剂的又足够高Retensionsunterschieden和相关联的高回收率至分离装置相对低的质量的差异固定化而放弃。反应混合物分离为高效生产的有机合成产品或光学活性的有机化合物的催化反应。

7. 发明申请

WO1997003091A1 PROCESS FOR PREPARING PEPTIDES AND N-CARBAMOYL-PROTECTED PEPTIDES 审中-公开
标题翻译：用于生产肽和N-甲酰保护肽
公开(公告)号：WO1997003091A1
公开(公告)日：1997-01-30
申请号：PCT/EP1996002782
申请日：1996-06-26
申请人： DEGUSSA AKTIENGESELLSCHAFT , BOMMARIUS, Andreas , DRAUZ, Karlheinz , EICHHORN, Uwe , JAKUBKE, Hans-Dieter , KOTTENHAHN, Matthias
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07K01/06
CPC分类号： C12P21/02 , C07K1/063 , Y02P20/55
摘要： The invention concerns a process for the enzymatic preparation of protected di- and oligopeptides and the separation of the protective groups used. The process according to the invention enables peptides to be synthesized simply and economically and the protective group to be separated carefully. The process comprises three reaction steps: 1. preparation of N-carbamoyl amino acid or N-carbamoyl amino acid derivatives; 2. formation of the peptide bond between the carbamoyl-protected electrophile and nucleophile; and 3. separation of the carbamoyl-protective group.
摘要翻译：描述了一种用于保护的二 - 和寡肽的酶制剂以及所用的保护基团的消除的处理。本发明的方法允许肽的容易的和低成本的合成以及温和除去保护基团。该方法涉及三个反应步骤：1. N-氨基甲酰基氨基酸或N-氨基甲酰基氨基酸衍生物的制备，形成2氨基甲酰基保护的亲电体亲核体和和3除去氨基甲酰基保护基团之间的肽键的。

8. 发明申请

WO1998022466A1 PROCESS FOR PREPARING MeO-Peg-PROTECTED DIHYDROQUININE OR DIHYDROQUINIDINE DERIVATIVES, NEW DIHYDROQUININE OR DIHYDROQUINIDINE DERIVATIVES AND THEIR USE 审中-公开
标题翻译：用于生产的MeO-PEG-保护或DIHYDROCHININ- DIHYDROCHINIDINDERIVATEN，新DIHYDROCHININ-或双氢及其用途
公开(公告)号：WO1998022466A1
公开(公告)日：1998-05-28
申请号：PCT/EP1997006396
申请日：1997-11-17
申请人： DEGUSSA AKTIENGESELLSCHAFT , BOLM, Carsten , GERLACH, Arne , DRAUZ, Karlheinz , BOMMARIUS, Andreas
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07B53/00 , C07D453/04
摘要： It is known that dihydroquinine or dihydroquinidine derivatives can be successfully used as ligands in the enantioselective dihydroxylation. The new disclosed ligand systems based on dihydroquinine/quinidine, unlike the prior art ligands, can be recycled after enantioselective dihydroxylation by precipitating and filtering the reaction medium, and be reused in the reaction. Also disclosed are the ligand systems (I) and (IV), processes for preparing the same and their use in the enantioselective dihydroxylation of double bonds.
摘要翻译：已知的是，Dihydrochinin-或二氢奎尼丁可以用作与成功不对称二羟基化的配体。根据本发明，基于二氢奎宁/奎尼丁新发现的配体体系从反应介质中回收，而相比之下，在那些根据通过沉淀和过滤的对映选择性的二羟基现有技术的配体描述并在反应中再次使用。配位体体系（I）和（IV）中，对于其制备方法，及其用于双键的对映选择性二羟基化。

9. 发明申请

WO1998022415A1 ENANTIOSELECTIVE CATALYTIC REDUCTION OF KETONES 审中-公开
标题翻译：处理该催化，对映选择性还原酮
公开(公告)号：WO1998022415A1
公开(公告)日：1998-05-28
申请号：PCT/EP1997006479
申请日：1997-11-20
申请人： DEGUSSA AKTIENGESELLSCHAFT , FORSCHUNGSZENTRUM JÜLICH GMBH , GIFFELS, Guido , FELDER, Marcel , KRAGL, Udo , WANDREY, Christian , DRAUZ, Karlheinz , BOMMARIUS, Andreas , BOLM, Carsten , DERRIEN, Nadine
发明人： DEGUSSA AKTIENGESELLSCHAFT , FORSCHUNGSZENTRUM JÜLICH GMBH
IPC分类号： C07C29/143
CPC分类号： C07C29/143 , C07B2200/07 , C07C33/22
摘要： Disclosed is a method of enantioselective catalytic reduction of ketones to chiral alcohols. So far, this reaction was made in batches. Expanding the catalysator by means of a polymer allows for a substantially continuous reaction to be obtained in a membrane reactor. The catalysator service life is significantly extended as compared with prior art.
摘要翻译：本发明涉及一种方法，用于催化，对映选择性还原酮的手性醇。到目前为止，这种反应是分批进行。特征在于，一个增加了的聚合物的方法中使用的催化剂，所以可以几乎连续地进行在膜反应器中的反应。相较于现有技术，而催化剂的寿命显着增加。

10. 发明申请

WO1997021650A1 PROCESS FOR RACEMIZATION OF N-ACETYL-D(L)-ALPHA-AMINOCARBOXYLIC ACIDS 审中-公开
标题翻译：过程对于N-乙酰基-D-（L）的外消旋 - α-氨基羧酸
公开(公告)号：WO1997021650A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005438
申请日：1996-12-05
申请人： DEGUSSA AKTIENGESELLSCHAFT , DRAUZ, Karlheinz , BOMMARIUS, Andreas , KARRENBAUER, Michael , KNAUP, Günter
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07B55/00
CPC分类号： C12P41/007 , C07C231/16 , C07C323/59 , C12P13/12
摘要： With known methods of racemizing N-acetyl-D(L)- alpha -aminocarboxylic acids in the non-aqueous state by heating them to temperatures above room temperature, significant quantities of by-products are formed, especially acetyl dipeptides. By converting at least a proportion of the N-acetyl-D(L)- alpha -aminocarboxylic acids to corresponding N-acetyl-D(L)- alpha -aminocarboxylic 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：在用于N-乙酰基-D-（L）的外消旋化的已知方法 - 的α-氨基羧酸中通过加热到比室温高的温度下在非水状态，有一个显著副产物的形成，特别是Acetyldipeptiden。之前或温度的作用期间在特征在于，至少所述N-乙酰基D（L）的一部分 - 的α-氨基羧酸为相应的N-乙酰基D（L） - 转移阿尔法-aminocarbonsäuresalze，所以能够消旋的更长的停留时间以允许在升高的温度下反应物而不副产物组分的增加（特别是乙酰化的二肽）中观察到。通过酶拆分获得的光学活性的氨基酸。

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