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    Process for preparing peptides and N-carbamoyl-protected peptides
    1.
    发明授权
    Process for preparing peptides and N-carbamoyl-protected peptides 失效
    制备肽和N-氨基甲酰保护肽的方法

    公开(公告)号：US06251625B1

    公开(公告)日：2001-06-26

    申请号：US09011859

    申请日：1998-04-03

    申请人： Andreas Bommarius ,  Karlheinz Drauz ,  Uwe Eichhorn ,  Hans-Dieter Jakubke ,  Matthias Kottenhahn

    发明人： Andreas Bommarius ,  Karlheinz Drauz ,  Uwe Eichhorn ,  Hans-Dieter Jakubke ,  Matthias Kottenhahn

    IPC分类号： C12P2106

    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 nucelophile; and 3. Separation of the carbamoyl-protective group.

    摘要翻译： 本发明涉及用于酶制备受保护的二肽和寡肽以及所用保护基的分离的方法。 根据本发明的方法使得肽可以简单和经济地合成，并且保护基被仔细分离。 该方法包括三个反应步骤：1.制备N-氨基甲酰基氨基酸或N-氨基甲酰基氨基酸衍生物; 氨基甲酰基保护的亲电子和生物素之间的肽键的形成; 和3.氨基甲酰基保护基的分离。

    Process for obtaining active L-.alpha.-amino carboxylic acids from corresponding racemic d, L-.alpha.-amino carboxylic acids
    7.
    发明授权
    Process for obtaining active L-.alpha.-amino carboxylic acids from corresponding racemic d, L-.alpha.-amino carboxylic acids 失效
    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。

    Process for preparing MeO-Peg-protected dihydroquinine or dihydroquinidine derivatives, new dihydroquinine or dihydroquinidine derivatives and their use
    10.
    发明授权
    Process for preparing MeO-Peg-protected dihydroquinine or dihydroquinidine derivatives, new dihydroquinine or dihydroquinidine derivatives and their use 失效
    制备MeO-Peg-保护的二氢奎尼丁或二氢奎尼丁衍生物的方法，新的二氢喹啉或二氢奎尼丁衍生物及其用途

    公开(公告)号：US06180551B2

    公开(公告)日：2001-01-30

    申请号：US09504183

    申请日：2000-02-15

    申请人： Carsten Bolm ,  Arne Gerlach ,  Karlheinz Drauz ,  Andreas Bommarius

    发明人： Carsten Bolm ,  Arne Gerlach ,  Karlheinz Drauz ,  Andreas Bommarius

    IPC分类号： C07D48704

    CPC分类号： C07D487/04 ,  C07B53/00 ,  C07D453/04

    摘要： Process for the formation of MeO-Peg-protected dihydroquinine or dihydro quinindine derivatives, new dihydroquinine-or dihyroquinidine derivatives as well as the use thereof. 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 medium. Also disclosed are the ligand systems (I) and (IV), process for preparing the same and their use in the enantioselective dihydroxiation of double bonds.

    摘要翻译： 形成MeO-Peg-保护的二氢喹啉或二氢喹啉衍生物，新的二氢喹啉或二氢喹啉衍生物的方法及其用途。 已知二氢奎尼丁或二氢奎尼丁衍生物可以成功地用作对映选择性二羟基化的配体。 与现有技术的配体不同，新公开的基于二氢喹啉/奎尼丁的配体体系可以通过沉淀和过滤反应介质在对映选择性二羟基化之后再循环，并在反应介质中重新使用。 还公开了配体体系（I）和（IV），其制备方法及其在双键对映体选择性二氢化中的用途。