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    GAMMA AMINO ACID BUILDING BLOCKS
    1.
    发明申请
    GAMMA AMINO ACID BUILDING BLOCKS 有权
    GAMMA氨基酸建筑块

    公开(公告)号：US20160280632A1

    公开(公告)日：2016-09-29

    申请号：US15174306

    申请日：2016-06-06

    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION

    Inventor： Samuel Helmer Gellman ,  Li Guo ,  Michael Giuliano

    IPC: C07C205/44 ,  C07C205/55 ,  C07C201/12

    CPC classification number: C07C205/44 ,  C07C201/12 ,  C07C205/55 ,  C07C233/48 ,  C07C237/24 ,  C07C269/00 ,  C07C271/24 ,  C07C271/66 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/56 ,  C07D211/60 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/1016 ,  C07K7/06

    Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained α-substituted-γ-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.).The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected γ-amino acid residues, which are essential for systematic conformational studies of γ-peptide foldamers. New methods are also provided to prepare other γ-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as α/γ-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.

    Abstract translation: 迈克尔加合物可以承受单个取代基或与羰基相邻的双取代基。 迈克尔加合物可以有效地转化为循环受限的受保护的γ-氨基酸残基，这对于γ-肽折叠物的系统构象研究至关重要。 还提供了新的方法来制备其它γ-氨基酸和肽。 这些新的构建块可用于制备在溶液中和固体状态下采用特定螺旋构象的折叠物，例如α/γ-肽折叠物。

    Gamma amino acid building blocks
    2.
    发明授权
    Gamma amino acid building blocks 有权
    伽玛氨基酸积木

    公开(公告)号：US09382291B2

    公开(公告)日：2016-07-05

    申请号：US14166007

    申请日：2014-01-28

    Applicant: Wisconsin Alumni Research Foundation

    Inventor： Samuel Helmer Gellman ,  Li Guo ,  Michael Giuliano

    IPC: C07K7/06 ,  C07C205/44 ,  C07C205/55 ,  C07C233/48 ,  C07C237/24 ,  C07C271/24 ,  C07D211/56 ,  C07D211/60 ,  C07K5/02 ,  C07C201/12 ,  C07C269/00 ,  C07C271/66 ,  C07K5/065 ,  C07K5/107

    CPC classification number: C07C205/44 ,  C07C201/12 ,  C07C205/55 ,  C07C233/48 ,  C07C237/24 ,  C07C269/00 ,  C07C271/24 ,  C07C271/66 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/56 ,  C07D211/60 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/1016 ,  C07K7/06

    Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained α-substituted-γ-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.).The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected γ-amino acid residues, which are essential for systematic conformational studies of γ-peptide foldamers. New methods are also provided to prepare other γ-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as α/γ-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.

    Abstract translation: 本发明提供了化合物和方法，例如，进行有机催化迈克尔加成醛到由脯氨酸衍生物催化的周期受限的硝基乙烯化合物以提供循环约束的α-取代的γ-硝基醛。 当使用手性吡咯烷催化剂时，可以使反应呈现对映选择性，允许以几乎光学纯的形式（例如，96至> 99％e.e。）的迈克尔加合物。 迈克尔加合物可以承受单个取代基或与羰基相邻的双取代基。 迈克尔加合物可以有效地转化为循环受限的受保护的γ-氨基酸残基，这对于γ-肽折叠物的系统构象研究至关重要。 还提供了新的方法来制备其它γ-氨基酸和肽。 这些新的构建块可用于制备在溶液中和固体状态下采用特定螺旋构象的折叠物，例如α/γ-肽折叠物。

    GAMMA AMINO ACID BUILDING BLOCKS
    3.
    发明申请
    GAMMA AMINO ACID BUILDING BLOCKS 有权
    GAMMA氨基酸建筑块

    公开(公告)号：US20150148523A1

    公开(公告)日：2015-05-28

    申请号：US14166007

    申请日：2014-01-28

    Applicant: Wisconsin Alumni Research Foundation

    Inventor： Samuel Helmer Gellman ,  Li Guo ,  Michael Giuliano

    IPC: C07K7/06 ,  C07C271/66 ,  C07C205/55 ,  C07C269/00 ,  C07K5/065 ,  C07K5/107 ,  C07C201/12 ,  C07C205/44 ,  C07C271/24

    CPC classification number: C07C205/44 ,  C07C201/12 ,  C07C205/55 ,  C07C233/48 ,  C07C237/24 ,  C07C269/00 ,  C07C271/24 ,  C07C271/66 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/56 ,  C07D211/60 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/1016 ,  C07K7/06

    Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained α-substituted-γ-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.).The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected γ-amino acid residues, which are essential for systematic conformational studies of γ-peptide foldamers. New methods are also provided to prepare other γ-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as α/γ-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.

    Abstract translation: 本发明提供了化合物和方法，例如，进行有机催化迈克尔加成醛到由脯氨酸衍生物催化的周期受限的硝基乙烯化合物以提供循环约束的α-取代的γ-硝基醛。 当使用手性吡咯烷催化剂时，可以使反应呈现对映选择性，允许以几乎光学纯的形式（例如，96至> 99％e.e。）的迈克尔加合物。 迈克尔加合物可以承受单个取代基或与羰基相邻的双取代基。 迈克尔加合物可以有效地转化为循环受限的受保护的γ-氨基酸残基，这对于γ-肽折叠物的系统构象研究至关重要。 还提供了新的方法来制备其它γ-氨基酸和肽。 这些新的构建块可用于制备在溶液中和固体状态下采用特定螺旋构象的折叠物，例如α/γ-肽折叠物。

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