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1. 发明申请

WO1997010203A1 METHOD OF PREPARING OPTICALLY ACTIVE 'alpha'-AMINO ACIDS AND 'alpha'-AMINO ACID DERIVATIVES 审中-公开
标题翻译：工艺制备光学活性的α-氨基酸和α-氨基衍生物
公开(公告)号：WO1997010203A1
公开(公告)日：1997-03-20
申请号：PCT/EP1996003984
申请日：1996-09-11
申请人： DEGUSSA AKTIENGESELLSCHAFT , ALTENBACH, Hans-Josef , KOTTENHAHN, Matthias , MATTHÄUS, Mike , VOGT, Annegret
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07C227/32
CPC分类号： C07D235/02 , C07C227/32
摘要： The invention concerns a novel method of preparing optically active amino acids and amino acid derivatives of general formula (I), in which *, X and R to R have the meanings given in the description. High yields of the enantiomerically-pure compounds of formula (I) are obtained from commercial (-)-menthol or (+)-menthol. The method is particularly suitable for preparing sterically demanding amino acids and amino acid derivatives.
摘要翻译：本发明涉及一种新的制备方法，其中* <1>具有光学活性的氨基酸和通式的氨基酸衍生物（I）中，X和R至R <4>在本说明书中给出的含义。（ - ） - 薄荷醇或（+） - 从市售起始薄荷醇，得到（I）在高产量式的对映体纯的化合物。该方法特别适合于生产大体积的氨基酸和氨基酸衍生物。

2. 发明申请

WO1996007634A1 PROCESS FOR REDUCING AMINO ACIDS AND DERIVATIVES THEREOF 审中-公开
标题翻译：一种用于减少氨基及其衍生物
公开(公告)号：WO1996007634A1
公开(公告)日：1996-03-14
申请号：PCT/EP1995003281
申请日：1995-08-17
申请人： DEGUSSA AKTIENGESELLSCHAFT , F. HOFFMANN-LA ROCHE AG , KOTTENHAHN, Matthias , DRAUZ, Karlheinz , HILPERT, Hans
发明人： DEGUSSA AKTIENGESELLSCHAFT , F. HOFFMANN-LA ROCHE AG
IPC分类号： C07C213/00
CPC分类号： C07D263/20 , C07C213/00 , C07C215/08 , C07C215/10 , C07C215/28
摘要： A process is disclosed for reducing amino acids and derivatives thereof. Compounds of formula (I), in which n = 0 or 1 and R , R , R , R , R and R have the meanings given in the description, are reduced to the corresponding amino alcohols of formula (II): the formula (I) compounds are converted in a first step, in at least one alcohol and with the addition of acid and heat, to an ester, this process producing a reaction mixture containing the ester; the ester is converted in a second reaction step with alkali or alkaline earth borohydride to compounds of formula II. By specifying that the second step be carried out without isolating the ester from the reaction mixture and by using alkali or alkaline earth borohydrides which are not activated, the invention facilitates the production from amino acids and their derivatives of the corresponding alcohols in a simple "single vessel" process, with high yields and in such a way as to preserve a given centre of chirality. Applications: synthesis components, preparation of optically active compounds, splitting of racemic compounds.
摘要翻译：式（I），其中n = 0或1的化合物，且R <1>，R <2>，R <3>，R <4>，R <5>和R <6>如说明书中所定义的含义，被还原成通式（II）的相应的氨基醇，式（I）的化合物中的至少一种醇的第一步先进行反应，同时加入酸并加热以形成酯，使含酯反应混合物，将得到的酯与碱金属或Erdalkaliborhydrid到（II）的化合物的第二步骤中反应。因为根据本发明，而不酯的隔离所述第二步骤从反应混合物中进行，并且碱金属或Erdalkaliborhydride使用哪个没有被激活，这是可能的，从氨基酸或氨基酸衍生物，在高一个简单的“一个锅煮”的方式相应的醇准备给如有必要，手性存在的产量。合成单元，显示光学活性化合物; 分辨率。

3. 发明申请

WO1995007928A1 PROCESS FOR PURIFYING 1-[N2-((S)-ETHOXYCARBONYL)-3-PHENYLPROPYL)-N6-TRIFLUOROACETYL]-L-LYSYL-L-PROLINE (LISINOPRIL(TFA)ETHYL ESTER) 审中-公开
标题翻译： PROCEDURE用于清洁1- [N <2> - （（S）乙氧基羰基）-3-苯基 - 丙基）-N <6> -TRIFLUORACEYTL〕-L-赖氨酰-L-脯氨酸（赖诺普利（TFA）乙基）
公开(公告)号：WO1995007928A1
公开(公告)日：1995-03-23
申请号：PCT/EP1994002760
申请日：1994-08-19
申请人： DEGUSSA AKTIENGESELLSCHAFT , KOTTENHAHN, Matthias , DRAUZ, Karlheinz
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07K05/02
CPC分类号： C07K5/0222 , A61K38/00
摘要： The invention relates to a process for purifying 1-[N -((S)-ethoxycarbonyl)-3-phenylpropyl)-N -trifluoroacetyl]-L-lysyl-L-proline (compound I) by extraction and crystallisation.
摘要翻译：本发明涉及一种用于纯化1- [N <2> - （（S） - 乙氧基羰基）-3-苯基丙基）-N <6> - 三氟乙酰基〕-L-赖氨酰-L-脯氨酸（化合物I）通过萃取和结晶。

4. 发明申请

WO1997002236A1 PROCESS FOR PRODUCING 'beta'-AMINO-'alpha'-HYDROXYCARBOXYLIC ACIDS AND DERIVATIVES THEREOF 审中-公开
标题翻译：用于生产β-氨基α-羟基羧酸和它们的衍生物
公开(公告)号：WO1997002236A1
公开(公告)日：1997-01-23
申请号：PCT/EP1996002573
申请日：1996-06-14
申请人： DEGUSSA AKTIENGESELLSCHAFT , STINGL, Klaus , KOTTENHAHN, Matthias , DRAUZ, Karlheinz
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07C231/12
CPC分类号： C07C213/00 , C07C227/26 , C07C269/06
摘要： Disclosed is a process for producing beta -amino- alpha -hydroxycarboxylic acid derivatives of general formula (2R,3S)- or (2S,3R)-N-(X,Y)-3-amino-2-hydroxy-3-phenyl-propionic acid-Z of formula (I), e.g. of (2R,3S)-3-amino-2-hydroxy-3-phenyl-propionic acid or (2R,3S)-N-benzoyl-3-amino-2-hydroxy-3-phenyl-propionic acid methylester. Compounds of type I are valuable intermediates in the total synthesis of taxols which can be used in the treatment of various forms of cancer.
摘要翻译：或（2S，3R）-N-（X，Y）-3-氨基-2-羟基-3-苯基 - 丙酸 - 一种制备通式的β-氨基α-羟基羧酸衍生物（2R，3S）过程（I）式-Z，例如（2R，3S）-3-氨基-2-羟基-3-苯基 - 丙酸或（2R，3S）-N-苯甲酰基-3-氨基-2-羟基-3-苯基丙酸甲酯。类型I的化合物在紫杉酚的总合成有价值的中间体，发现的各种癌症使用的治疗。

5. 发明申请

WO1996007642A1 PROCESS FOR PRODUCING A 'beta'-AMINO ALCOHOL 审中-公开
标题翻译：用于生产的β-氨基醇
公开(公告)号：WO1996007642A1
公开(公告)日：1996-03-14
申请号：PCT/EP1995003280
申请日：1995-08-17
申请人： F. HOFFMANN-LA ROCHE AG , DEGUSSA AKTIENGESELLSCHAFT , KOTTENHAHN, Matthias , DRAUZ, Karlheinz , HILPERT, Hans
发明人： F. HOFFMANN-LA ROCHE AG , DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07D217/26
CPC分类号： C07D263/20 , C07C271/22 , C07D217/26 , C07D263/24 , C07D413/06
摘要： A process for producing 2-[3(S)-amino-2-(R)-hydroxyl-4-phenyl butyl]-N-tert.butyl decahydro-(4aS, 8aS)-isoquinoline-e(S)-carboxamide of the formula (I) via 3(S)-[lower alkoxy carbonyl amino, phenoxy carbonyl amino or benzyl oxycarbonyl amino]-2-hydroxy-4-phenyl butyric acid and process for producing said acid.
摘要翻译：一种用于2- [3（S） - 氨基-2（R） - 羟基-4-苯基丁基〕-N-叔丁基 - 十氢 - （4AS，8AS）下式的异喹啉-3（S） - 甲酰胺的制备方法（I）通过3（S） - [Niederalkoxycarbonylamino-，苯氧基羰基或苄氧基羰基] -2-羟基-4-苯基丁酸和使后者酸的方法。

6. 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。

7. 发明申请

WO1995014021A1 HYDANTOIN DERIVATIVES AND THEIR USE AS BLEACH ACTIVATORS 审中-公开
标题翻译：乙内酰脲衍生物及其作为漂白活化剂使用
公开(公告)号：WO1995014021A1
公开(公告)日：1995-05-26
申请号：PCT/EP1994002568
申请日：1994-08-03
申请人： DEGUSSA AKTIENGESELLSCHAFT , DEL GROSSO, Michael , TANNER, Herbert , KOTTENHAHN, Matthias , THIELE, Georg
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C11D3/392
摘要： The invention relates to hydantoin derivatives of general formula (I) in which n is 1 or 2 and R is H, alkoxycarbonyl or acyl. 2-N-acyldihydropyrrolo[1,2-climidazole-1,3,5-trione is the preferred derivative, the acyl groups being a lower alkanoyl or phenyl. These hydantoin derivatives can be used as activators for inorganic peroxy compounds and exhibit a bleaching power which is several times that of tetraacetylethylenediamine (TAED). The invention also concerns bleaching, washing, cleaning and disinfecting agents containing the activators proposed.
摘要翻译：本发明涉及通式（I）其中n为1或2，且R为H，烷氧基羰基或酰基的新颖乙内酰脲衍生物。 2-N-酰基 - 二氢 - 吡咯并[1,2-C]咪唑-1,3,5-三酮与酰基等于低级链烷酰基或苯基是优选的。乙内酰脲衍生物可被用作活化剂为无机过氧化合物，并显示这往往超过TAED的漂白能力。还涉及含活化剂 - 新颖漂白洗涤剂，清洁剂和消毒剂。

8. 发明申请

WO1997012881A1 PROCESS FOR THE CONTINUOUS PRODUCTION OF BASIC CYCLIC OPTICALLY ACTIVE 'alpha'-AMINO ACIDS 审中-公开
标题翻译： PROCESS FOR碱性连续生产，环状的，光学活性的α-氨基酸
公开(公告)号：WO1997012881A1
公开(公告)日：1997-04-10
申请号：PCT/EP1996004073
申请日：1996-09-18
申请人： DEGUSSA AKTIENGESELLSCHAFT , KOTTENHAHN, Matthias , STINGL, Klaus , DRAUZ, Karlheinz
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07D241/04
CPC分类号： C07D241/04
摘要： The invention pertains to a process for the continuous production of basic cyclic optically active alpha -amino acids of general formula (I) by continuous racemate splitting via diastereomeric salt pairs with re-racemisation of the residual amino acid or amino acid derivative in the mother liquor with the aid of an optically active acid.
摘要翻译：一种用于生产基本的，环状的，通过经由Reracemisierung下非对映盐对残留在使用光学活性的酸的氨基酸或氨基酸衍生物的母液的连续外消旋体拆分通式（I）的光学活性α-氨基酸的过程。

9. 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.

10. 发明申请

WO1997019890A1 COATED SODIUM PERCARBONATE PARTICLES, PROCESS FOR THE PRODUCTION THEREOF AND USE THEREOF 审中-公开
标题翻译：包衣酸钙颗粒，其生产方法及其用途
公开(公告)号：WO1997019890A1
公开(公告)日：1997-06-05
申请号：PCT/EP1996004986
申请日：1996-11-14
申请人： DEGUSSA AKTIENGESELLSCHAFT
发明人： DEGUSSA AKTIENGESELLSCHAFT , SCHÜTTE, Rüdiger , BEWERSDORF, Martin , KLASEN, Claas-Jürgen
IPC分类号： C01B15/10
CPC分类号： C11D3/046 , C01B15/106 , C11D3/3942 , C11D17/0039 , Y10T428/2991
摘要： In order to increase active oxygen stability, sodium percarbonate is coated with single or multiple layers of various substances. Sodium percarbonate particles coated according to the invention consist of a core of sodium percarbonate fluidised bed spray granulate and sodium sulphate, which may be partially hydrated, as the sole constituent of a single coating layer. The particles according to the invention exhibit both elevated active oxygen stability and very good ensilability. The coating layer is applied by spraying an aqueous Na2SO4 solution onto the particles to be coated, which were themselves produced by fluidised bed spray granulation, in a fluidised bed and vaporising water at a fluidised bed temperature of 35 to 100 DEG C.
摘要翻译：为了提高活性氧的稳定性，过碳酸钠被单层或多层各种物质涂覆。根据本发明涂覆的过碳酸钠颗粒由可以部分水合的过碳酸钠流化床喷雾颗粒和硫酸钠的核心组成，作为单一涂层的唯一成分。根据本发明的颗粒显示升高的活性氧稳定性和非常好的可靠性。通过在流化床喷雾造粒本身产生的待涂覆颗粒上，在流化床温度为35-100℃的气态水中喷洒Na 2 SO 4水溶液来涂覆涂层。

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