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    Diketopiperazine forming dipeptidyl linker
    7.
    发明授权
    Diketopiperazine forming dipeptidyl linker 有权
    二酮哌嗪形成二肽基接头

    公开(公告)号：US08802819B2

    公开(公告)日：2014-08-12

    申请号：US13881883

    申请日：2011-10-20

    申请人： Fernando Albericio ,  Michèle Cristau ,  Matthieu Giraud ,  Miriam Gongora Benitez ,  Judit Tulla-Puche

    发明人： Fernando Albericio ,  Michèle Cristau ,  Matthieu Giraud ,  Miriam Gongora Benitez ,  Judit Tulla-Puche

    IPC分类号： C07K1/06 ,  C07K1/02 ,  C07K1/04 ,  C07K5/068

    CPC分类号： C07K1/068 ,  C07K1/04 ,  C07K1/062 ,  C07K5/06086 ,  C08F112/08 ,  Y02P20/55

    摘要： The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided. The invention relates further to a method for the preparation of such specifically protected fragment C-PEP by SPPS by using a linker comprising a specific dipeptide and HG for connecting the growing peptide chain to the resin, which linker forms said DKP group, when the peptide fragment C-PEP is cleaved from the supporting resin; and further to the intermediates of the preparation method.

    摘要翻译： 本发明涉及一种N-末端肽片段PEP-N和C-末端肽片段C-PEP的均相溶液相肽合成（HSPPS）的方法，其中携带特异性二酮哌嗪（DKP）的C-PEP包含C- 末端保护基，其含有句柄组HG，其中HG连接到肽片段的C末端; 因此，作为常规使用的C末端保护基可以从肽中选择性地切割含有C末端保护基的这种特定的DKP。 通过使用包含C末端保护基的该DKP和HG，可以避免基于HSPPS和固相肽合成（SPPS）的组合的收敛肽合成中的某些方法步骤。 本发明进一步涉及通过使用包含特异性二肽和HG的连接体将这种特异性保护的片段C-PEP制备成用于将生长中的肽链连接到树脂上的方法，该连接体形成所述DKP基团，当肽 片段C-PEP与支撑树脂分离; 并且还涉及制备方法的中间体。

    Diketopiperazine Forming Dipeptidyl Linker
    8.
    发明申请
    Diketopiperazine Forming Dipeptidyl Linker 有权
    二酮哌嗪形成二肽基连接子

    公开(公告)号：US20140094567A1

    公开(公告)日：2014-04-03

    申请号：US13881883

    申请日：2011-10-20

    申请人： Fernando Albericio ,  Michèle Cristau ,  Matthieu Giraud ,  Miriam Gongora Benitez ,  Judit Tulla-Puche

    发明人： Fernando Albericio ,  Michèle Cristau ,  Matthieu Giraud ,  Miriam Gongora Benitez ,  Judit Tulla-Puche

    IPC分类号： C07K1/06

    CPC分类号： C07K1/068 ,  C07K1/04 ,  C07K1/062 ,  C07K5/06086 ,  C08F112/08 ,  Y02P20/55

    摘要： The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided. The invention relates further to a method for the preparation of such specifically protected fragment C-PEP by SPPS by using a linker comprising a specific dipeptide and HG for connecting the growing peptide chain to the resin, which linker forms said DKP group, when the peptide fragment C-PEP is cleaved from the supporting resin; and further to the intermediates of the preparation method.

    摘要翻译： 本发明涉及一种N-末端肽片段PEP-N和C-末端肽片段C-PEP的均相溶液相肽合成（HSPPS）的方法，其中携带特异性二酮哌嗪（DKP）的C-PEP包含C- 末端保护基，其含有句柄组HG，其中HG连接到肽片段的C末端; 因此，作为常规使用的C末端保护基可以从肽中选择性地切割含有C末端保护基的这种特定的DKP。 通过使用包含C末端保护基的该DKP和HG，可以避免基于HSPPS和固相肽合成（SPPS）的组合的收敛肽合成中的某些方法步骤。 本发明进一步涉及通过使用包含特异性二肽和HG的连接子将该特异性保护的片段C-PEP制备成用于将生长中的肽链连接到树脂上的方法，该接头形成所述DKP基团，当肽 片段C-PEP与支撑树脂分离; 并且还涉及制备方法的中间体。