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    Process for the preparation of retro-inverso peptides and new intermediates thereof
    1.
    发明公开
    Process for the preparation of retro-inverso peptides and new intermediates thereof 失效
    Verfahren zur Herstellung von Retro-Inverso-Peptiden und dessen Zwischenprodukte。

    公开(公告)号：EP0375040A2

    公开(公告)日：1990-06-27

    申请号：EP89203194.9

    申请日：1989-12-14

    申请人： SCLAVO S.p.A.

    发明人： Pinori, Massimo ,  Centini, Felice ,  Verdini, Antonio Silvio

    IPC分类号： C07K1/02 ,  C07K1/12 ,  C07K5/02 ,  C07D319/06

    CPC分类号： C07K1/02 ,  C07D319/06 ,  C07K5/0212

    摘要： A method of synthesis of a partially retro-inverso peptide incorporating at least one malonyl residue of formula (III)
    -CO- H-CO-      (III)

    wherein R represents the side chain of an α-amino acid, is described which is characterized in that said malonyl residue is incorporated by condensing a 5-substituted-2,2-dimethyl-1,3-dioxane-4,6-dione of formula (VI)
    wherein R′ is the side-chain R wherein the functional groups, if any, are suitably protected, with an amino acid, amino acid amide, peptide fragment, or pseudo-peptide fragment wherein the terminal carboxyl group, if present, and the possible side-chain functionalities are suitably protected and the reactive amino group is tri-alkyl-silylated.
    The new compounds of formula (VI) and a process for the preparation of a partially retro-inverso tuftsin analog which involves use of said method and said intermediate are also described and claimed.

    摘要翻译： 一种合成部分逆转肽的方法，其包含至少一种式（III）-CO-H-CO-（III）的丙二酰残基，其中R表示α-氨基酸的侧链，其是 其特征在于所述丙二酰残基通过将式（VI）的5-取代-2,2-二甲基-1,3-二恶烷-4,6-二酮缩合成CHEM，其中R min是侧链R，其中 如果有的话，官能团被适当地保护，其中氨基酸，氨基酰胺，肽片段或假肽片段，其中如果存在末端羧基，并且可能的侧链官能团被适当地保护，并且反应性 氨基是三烷基甲硅烷基化的。 还描述和要求保护新的式（VI）化合物和涉及使用所述方法和所述中间体的部分逆转型绒毛蛋白类似物的制备方法。

    New gem-diamino derivatives and their use in the synthesis of retro-inverso peptides
    3.
    发明公开
    New gem-diamino derivatives and their use in the synthesis of retro-inverso peptides 失效
    Gem-diamino-Derivate und ihre Verwendung bei der Herstellung von Retro-Inverso-Peptiden。

    公开(公告)号：EP0384523A2

    公开(公告)日：1990-08-29

    申请号：EP90200352.4

    申请日：1990-02-16

    申请人： ENIRICERCHE S.p.A. ,  SCLAVO S.p.A.

    发明人： Gazerro, Laura ,  Pinori, Massimo ,  Verdini, Antonio Silvio

    IPC分类号： C07C235/10 ,  C07C235/78 ,  C07K1/06 ,  C07K5/02

    CPC分类号： C07K1/063 ,  C07C235/20 ,  C07C235/34 ,  C07C237/20 ,  C07C237/22 ,  C07C271/22 ,  C07K5/0212

    摘要： This invention relates to new gem-diamino derivatives of general formula (I)
    where

    R is the side chain of an amino acid, of which any functional groups are suitably protected, and
    X is an acyl group chosen from the group consisting of 2-nitro-benzoyl, 4-chloro-butyryl, acetoacetyl, 4-bromo-butyryl, (2-nitro-phenoxy)-acetyl and 2-methyl-2-(2'-nitro-phenoxy)propionyl, of use in introducing gem-diamino residues into retro-inverso peptides. The invention further relates to a method for the synthesis of retro-inverso peptides in which the gem-diamino residue or residues are introduced using the new compound (I).

    摘要翻译： 本发明涉及通式（I）X-NH-H-NH 2（I）的新的偕二氨基衍生物，其中R是氨基酸的侧链，其中任何官能团都被适当地保护，X是 选自2-硝基 - 苯甲酰基，4-氯 - 丁酰基，乙酰乙酰基，4-溴 - 丁酰基，（2-硝基 - 苯氧基） - 乙酰基和2-甲基-2-（2min - 苯氧基）丙酰基，用于将偕二氨基残基引入逆转肽。 本发明还涉及一种用于合成其中使用新化合物（I）引入偕二氨基残基或残基的逆转肽的方法。

    Process for the preparation of retro-inverso peptides and new intermediates thereof
    5.
    发明公开
    Process for the preparation of retro-inverso peptides and new intermediates thereof 失效
    制备逆转录酶的方法及其新的中间体

    公开(公告)号：EP0375040A3

    公开(公告)日：1991-07-03

    申请号：EP89203194.9

    申请日：1989-12-14

    申请人： SCLAVO S.p.A.

    发明人： Pinori, Massimo ,  Centini, Felice ,  Verdini, Antonio Silvio

    IPC分类号： C07K1/02 ,  C07K1/12 ,  C07K5/02 ,  C07D319/06

    CPC分类号： C07K1/02 ,  C07D319/06 ,  C07K5/0212

    摘要： A method of synthesis of a partially retro-inverso peptide incorporating at least one malonyl residue of formula (III)
    -CO- H-CO-      (III)
    wherein R represents the side chain of an α-amino acid, is described which is characterized in that said malonyl residue is incorporated by condensing a 5-substituted-2,2-dimethyl-1,3-dioxane-4,6-dione of formula (VI)
    wherein R′ is the side-chain R wherein the functional groups, if any, are suitably protected, with an amino acid, amino acid amide, peptide fragment, or pseudo-peptide fragment wherein the terminal carboxyl group, if present, and the possible side-chain functionalities are suitably protected and the reactive amino group is tri-alkyl-silylated. The new compounds of formula (VI) and a process for the preparation of a partially retro-inverso tuftsin analog which involves use of said method and said intermediate are also described and claimed.