发明公开
EP0375040A2 Process for the preparation of retro-inverso peptides and new intermediates thereof
失效
Verfahren zur Herstellung von Retro-Inverso-Peptiden und dessen Zwischenprodukte。
- 专利标题： Process for the preparation of retro-inverso peptides and new intermediates thereof
- 专利标题（中）： Verfahren zur Herstellung von Retro-Inverso-Peptiden und dessen Zwischenprodukte。
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申请号： EP89203194.9申请日： 1989-12-14
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公开(公告)号： EP0375040A2公开(公告)日： 1990-06-27
- 发明人: Pinori, Massimo , Centini, Felice , Verdini, Antonio Silvio
- 申请人： SCLAVO S.p.A.
- 申请人地址： Via Fiorentina 1 I-53100 Siena IT
- 专利权人： SCLAVO S.p.A.
- 当前专利权人： SCLAVO S.p.A.
- 当前专利权人地址： Via Fiorentina 1 I-53100 Siena IT
- 代理机构： Gervasi, Gemma, Dr.
- 优先权： IT2309888 19881223
- 主分类号： C07K1/02
- IPC分类号： C07K1/02 ; C07K1/12 ; C07K5/02 ; C07D319/06
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.
-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.
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