申请人:ANIC S.p.A.
公开号:EP0084691A1
公开(公告)日:1983-08-03
This invention relates to a new method for preparing N-mono-acylated gem-diamino derivatives of general formula I from an aminoacid, hydroxyacid, peptide or depsipeptide residue with the terminal -NH2 or -OH groups protected
In particular, the method according to the present invention consists of directly converting primary linear aminoacid, hydroxyacid, peptide or depsipeptide amides protected at the terminal -NH2 or -OH, of general formula II
into the corresponding primary amines of general formula I by reacting with I,I-bis(trifluoroacetoxy)iodobenzene.
The derivatives of general formula I are important intermediates in the synthesis of biologically active retro-inverso peptides which are stable to enzymatic degradation.
本发明涉及一种新方法,用于从末端-NH2 或-OH 基团受保护的氨基酸、羟基酸、肽或去肽残基制备通式 I 的 N-单酰化 gem-二氨基衍生物。
具体而言,根据本发明的方法包括将通式 II 的末端 -NH2 或 -OH 受保护的伯胺、羟基酸、肽或副肽酰胺直接转化为通式 II 的相应伯胺
与 I,I-双(三氟乙酰氧基)碘苯反应,直接转化为相应的通式 I 伯胺。
通式 I 的衍生物是合成对酶降解稳定的具有生物活性的反转录肽的重要中间体。