Acid-labile anchor groups for the synthesis of peptide amides by a
solid-phase method
    30.
    发明授权
    Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method 失效
    用于通过固相法合成肽类化合物的酸可溶性锚固剂组

    公开(公告)号:US5124478A

    公开(公告)日:1992-06-23

    申请号:US287213

    申请日:1988-12-20

    摘要: The invention relates to new compounds of the formula ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.8)-alkyl, R.sup.2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R.sup.3 denotes hydrogen or (C.sub.1 -C.sub.4)-alkyl, and Y.sup.1 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy or --O--(CH.sub.2).sub.n --COOH (with n=1 to 6), with one of these radicals being --O--(CH.sub.2).sub.n --COOH, or Y.sup.1, Y.sup.2 and Y.sup.5 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-alkoxy, Y.sup.3 denotes hydrogen or (C.sub.1 -C.sub.8)-alkoxy and Y.sup.4 denotes --(CH.sub.2).sub.n --COOH or --NH--CO--(CH.sub.2).sub.n --COOH (with n=1 to 6).Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.

    摘要翻译: 本发明涉及新的式(I)化合物,其中R 1表示(C 1 -C 8) - 烷基,R 2表示被氨基保护基团保护的氨基酸残基,该氨基酸残基可用弱酸或碱 ,或表示可用弱酸或碱取代的氨基保护基,R3表示氢或(C1-C4) - 烷基,Y1-Y9表示相同或不同的基团,氢,(C1-C4) - 烷基,(C1 -C(O) - 烷氧基或-O-(CH 2)n -COOH(n = 1至6),其中一个基团是-O-(CH 2)n -COOH,或者Y 1,Y 2和Y 5 -Y 9表示相同 或(C 1 -C 4) - 烷氧基,Y 3表示氢或(C 1 -C 8) - 烷氧基,Y 4表示 - (CH 2)n -COOH或-NH-CO-(CH 2) )n-COOH(n = 1〜6)。 描述了通过使用这些新化合物(间隔物)的固相方法制备方法和肽酰胺的合成方法。