Method for the aminolysis of activated esters in the presence of N-hydroxy compounds as catalysts
    1.
    发明授权
    Method for the aminolysis of activated esters in the presence of N-hydroxy compounds as catalysts 失效
    在N-羟基化合物作为催化剂存在下活化酯的氨解方法

    公开(公告)号:US3872074A

    公开(公告)日:1975-03-18

    申请号:US26444172

    申请日:1972-06-20

    Applicant: HOECHST AG

    CPC classification number: C07K5/06043 A61K38/00 C07K1/10 C07K14/625 C07K14/695

    Abstract: A process for the manufacture of peptides by reacting a protected amino acid or a protected peptide ester with an optionally protected amino acid or a peptide having a free amino group, which may be bound to a polymer support, by adding a heterocyclic compound of the formula

    D R A W I N G
    WHEREIN X stands for the groups C O, C S or -N and X and N are members of a 5- or 6-membered heterocyclic ring optionally substituted and fused with a benzene nucleus and/or optionally containing 1 or 2 further hetero atoms, and the pK-value whereof lies between 3.7 and 4.2, as catalysts for the condensation.

    Abstract translation: 通过将受保护的氨基酸或受保护的肽酯与任选保护的氨基酸或具有游离氨基的肽(其可以结合到聚合物载体)反应,通过加入式 其中X代表基团C = O,C = S或-N =且X和N是任选被取代并与苯核稠合的5或6元杂环的成员和/或任选地含有1或2个 杂原子,其pK值在3.7和4.2之间,作为缩合的催化剂。

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