申请人:Hoechst Aktiengesellschaft
公开号:US04922015A1
公开(公告)日:1990-05-01
The invention relates to new compounds of the formula ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.8)-alkyl or optionally substituted (C.sub.6 -C.sub.14)-aryl, R.sup.2 denotes hydrogen or an amino acid residue which is protected by an amino protective group which can be cleaved off 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), one of these radicals being -O-(CH.sub.2).sub.n -COOH. A process for the preparation thereof and the synthesis of peptide amides by means of a solid phase method using these new compounds (spacers) are described.
该发明涉及以下结构的新化合物##STR1##其中R.sup.1表示(C.sub.1 -C.sub.8)-烷基或可选择取代的(C.sub.6 -C.sub.14)-芳基,R.sup.2表示氢或由氨基保护基保护的氨基酸残基,该保护基可通过弱酸或碱脱除,R.sup.3表示氢或(C.sub.1 -C.sub.4)-烷基,Y.sup.1 -Y.sup.9表示相同或不同的基团氢、(C.sub.1 -C.sub.4)-烷基、(C.sub.1 -C.sub.4)-烷氧基或-O-(CH.sub.2).sub.n -COOH(其中n=1至6),其中一个基团为-O-(CH.sub.2).sub.n -COOH。描述了制备这些化合物(间隔物)的方法以及利用这些新化合物(间隔物)采用固相法合成肽酰胺。