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18 条记录 (耗时 0.026 秒)

    Enzymatic Conversion of Oligopeptide Amides to Oligopeptide Alkylesters
    1.
    发明申请
    Enzymatic Conversion of Oligopeptide Amides to Oligopeptide Alkylesters 审中-公开
    寡肽酰胺对寡肽烷基酯的酶转化

    公开(公告)号：US20090298118A1

    公开(公告)日：2009-12-03

    申请号：US12083285

    申请日：2006-10-19

    申请人： Peter Jan Leonard Mario Quaedflieg ,  Theodorus Sonke ,  Gerardus Karel Maria Verzijl ,  Roel Wim Wiertz

    发明人： Peter Jan Leonard Mario Quaedflieg ,  Theodorus Sonke ,  Gerardus Karel Maria Verzijl ,  Roel Wim Wiertz

    IPC分类号： C12P21/00

    CPC分类号： C12P21/00

    摘要： The present invention relates to enzymatic oligopeptide synthesis in the N→C direction, in particular to a process for the preparation of an optionally N-protected oligopeptide C-terminal alkylester comprising the step of reacting the corresponding optionally N-protected oligopeptide C-terminal carboxyamide with an alkyl alcohol, preferably methanol, in the presence of a peptide amidase. The formed C-terminal alkylester can subsequently be used for the coupling with another amino acid residue or oligopeptide. Therefore, inventors have found a very advantageous process for the preparation of oligopeptides.

    摘要翻译： 本发明涉及在N-> C方向的酶促寡肽合成，特别涉及制备任选N-保护的寡肽C端烷基酯的方法，该方法包括使相应的任选N-保护的寡肽C末端 羧酰胺与烷基醇，优选甲醇在肽酰胺酶存在下反应。 形成的C-末端烷基酯随后可用于与另一氨基酸残基或寡肽的偶联。 因此，发明人已经发现了制备寡肽的非常有利的方法。

    Process for the preparation of compounds with enhanced optical purity
    6.
    发明授权
    Process for the preparation of compounds with enhanced optical purity 失效
    具有增强的光学纯度的化合物的制备方法

    公开(公告)号：US07018817B1

    公开(公告)日：2006-03-28

    申请号：US09869088

    申请日：1999-12-17

    申请人： Peter Jan Leonard Mario Quaedflieg ,  Theodorus Sonke ,  Adolf Fritz Volker Wagner

    发明人： Peter Jan Leonard Mario Quaedflieg ,  Theodorus Sonke ,  Adolf Fritz Volker Wagner

    IPC分类号： C12P21/06 ,  C12P13/22

    CPC分类号： C12P41/007 ,  C12P13/04

    摘要： Process for the preparation of a compound with enhanced optical purity wherein a mixture of the enantiomers of a chiral compound of formula 1 wherein: R1 represents an alkyl or an aryl group R2 represents H, an alkyl or an aryl group Y represents an alkyl group, an aryl group, (CH2)nCOOH, (CH2)n—COOR, (CH2)n—CONRR′, CH2OH, or C≡N wherein R and R′ independently represent H, an alkyl or aryl group, and n represents 0 or 1, is brought into contact with an enzyme having peptide deformylase activity with a bivalent metal ion as a cofactor wherein the metal is chosen from the groups 5–11 of the periodic system, or for the preparation of a formylated compound with enhanced optical purity from a mixture of the enantiomers of the corresponding not formulated chiral compound in the presence of a formylation agent. Preferably the peptide deformylase is chosen from the class EC 3.5.2.27 or EC 3.5.1.31, and contains the sequences of (I) HEXXH, (ii) EGCLS and (iii) GXGXAAXQ. The bivalent metal may be chosen from the group of Fe, Ni, Mn and Co, preferably Ni or Fe.

    摘要翻译： 用于制备具有增强的光学纯度的化合物的方法，其中式1的手性化合物的对映异构体的混合物，其中：R 1表示烷基或芳基R 2 >表示H，烷基或芳基Y表示烷基，芳基，（CH 2）n COOH，（CH 2）2 CO （CH 2）n CO 2，-CONRR'，CH 2 OH或C≡ N其中R和R'独立地表示H，烷基或芳基，n表示0或1与具有肽变形酶活性的酶与二价金属离子作为辅因子进行接触，其中金属选自 5-11，或在甲酰化剂存在下由相应的未配制的手性化合物的对映异构体的混合物制备具有增强的光学纯度的甲酰化的化合物。 优选地，肽变性酶选自EC 3.5.2.27或EC 3.5.1.31，并且包含（I）HEXXH，（ii）EGCLS和（iii）GXGXAAXQ的序列。 二价金属可以选自Fe，Ni，Mn和Co，优选Ni或Fe。

    Peptide synthesis using enzymatic activation and coupling
    8.
    发明授权
    Peptide synthesis using enzymatic activation and coupling 有权
    使用酶活化和偶联的肽合成

    公开(公告)号：US08883444B2

    公开(公告)日：2014-11-11

    申请号：US13129663

    申请日：2009-11-19

    申请人： Peter Jan Leonard Mario Quaedflieg ,  Timo Nuijens ,  Claudia Cusan ,  Catharina Hubertina Maria Schepers

    发明人： Peter Jan Leonard Mario Quaedflieg ,  Timo Nuijens ,  Claudia Cusan ,  Catharina Hubertina Maria Schepers

    IPC分类号： C12P21/06 ,  C07K1/02 ,  C12P21/02

    CPC分类号： C12P21/02 ,  C07K1/02 ,  C07K1/026

    摘要： The invention relates to a method for synthesizing a peptide by enzymatically preparing an ester or thioester from (i) an N-terminal protected amino acid or an N-terminal protected peptide where either can have a protected C-terminal ester group and (ii) an alcohol represented by the formula HO—CX2—Z or a thiol represented by the formula HS—CX2—Z, each X independently representing a halogen atom or a hydrogen atom; and Z represents an electron withdrawing group comprising at least one sp3-hybridized carbon comprising at least two substituents comprising a heteroatom directly attached to the at least one sp3-hybridized carbon or at least one sp2-hybridized carbon comprising one or two substituents comprising a heteroatom directly attached to the at least one sp2-hybridized carbon, and enzymatically coupling the prepared ester or thioester with an optionally C-terminal protected amino acid or with an optionally C-terminal protected peptide in a medium comprising 2 wt. % water or less.

    摘要翻译： 本发明涉及一种通过从（i）N-末端保护的氨基酸或N-末端保护的肽（其中可以具有受保护的C端酯基）酶促制备酯或硫酯来合成肽的方法，和（ii） 由式HO-CX2-Z表示的醇或由式HS-CX2-Z表示的硫醇，每个X独立地表示卤素原子或氢原子; Z代表包含至少一个sp3-杂化的碳的吸电子基团，其包含至少两个包含直接连接至至少一个sp3杂化的碳原子的杂原子的至少两个取代基或至少一个包含一个或两个包含杂原子的取代基的sp2杂化的碳 直接连接到至少一个sp2杂交的碳上，并将制备的酯或硫酯与任选C末端保护的氨基酸或任选C末端保护的肽在包含2wt。 ％以下水。