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    METHOD FOR PRODUCING NITRO COMPOUND
    44.
    发明申请
    METHOD FOR PRODUCING NITRO COMPOUND 有权
    生产硝基化合物的方法

    公开(公告)号：US20160318846A1

    公开(公告)日：2016-11-03

    申请号：US15107872

    申请日：2014-12-15

    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED

    Inventor： Yuya YOSHIMOTO ,  Tatsuya TORIUMI ,  Yuta NAGASHIMA

    IPC: C07C201/12 ,  C07C213/02 ,  C07C205/34

    CPC classification number: C07C201/12 ,  C07C205/34 ,  C07C213/02 ,  C07C217/76

    Abstract: A nitro compound represented by formula (1) which is a raw material for producing a compound represented by formula (7) can be produced by reacting at least one type selected from the group consisting of a compound represented by formula (2), a compound represented by formula (3), and a compound represented by formula (3′) with a compound represented by formula (4). [In the formula, R1, R2, R3, and R4 are each independently a hydrogen atom, etc., X1 and X2 are each independently a chlorine atom, etc., R6, R7, R8, and R9 are a hydrogen atom, etc., provided that X1, X2, R6, R7, R8, and R9 are not all the same, X3, X4, and X5 are a halogen atom, R10 is a nitro group, etc., R5 is an alkyl group having 1 to 12 carbon atoms, etc., and M is an alkali metal atom.]

    GAMMA AMINO ACID BUILDING BLOCKS
    45.
    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。

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