申请人:Hoechst Aktiengesellschaft
公开号:US05124478A1
公开(公告)日:1992-06-23
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.
该发明涉及公式##STR1##中的新化合物,其中R.sup.1表示(C.sub.1 -C.sub.8)-烷基,R.sup.2表示氨基酸残基,其用尿素保护基保护,可以用弱酸或碱消除,或表示可以用弱酸或碱消除的氨基保护基,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(n=1至6),其中其中一个基团为--O--(CH.sub.2).sub.n --COOH,或Y.sup.1、Y.sup.2和Y.sup.5 -Y.sup.9表示相同或不同的基团氢,(C.sub.1 -C.sub.4)-烷基或(C.sub.1 -C.sub.4)-烷氧基,Y.sup.3表示氢或(C.sub.1 -C.sub.8)-烷氧基,Y.sup.4表示--(CH.sub.2).sub.n --COOH或--NH--CO--(CH.sub.2).sub.n --COOH(n=1至6)。描述了制备这些化合物(间隔物)的方法以及使用这些新化合物(间隔物)通过固相法合成肽酰胺的方法。