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1. 发明授权

EP0152977B1 Process for the preparation of L-alpha-aminoacids 失效
标题翻译：制备L-阿尔法 - 氨基酸的方法
公开(公告)号：EP0152977B1
公开(公告)日：1988-07-20
申请号：EP85200098.3
申请日：1985-01-31
申请人： SCLAVO S.p.A.
发明人： Olivieri, Roberto , Eletti Bianchi, Giancarlo , Fascetti, Eugenio , Centini, Felice
IPC分类号： C12P13/04 , C12P13/06 , C12P13/22 , C12P13/08 , C07C101/02 , C07C101/08
CPC分类号： C12P41/009 , C12P17/10

2. 发明授权

EP0375040B1 Process for the preparation of retro-inverso peptides and new intermediates thereof 失效
标题翻译：一种制备逆反肽，及其中间产物的过程。
公开(公告)号：EP0375040B1
公开(公告)日：1994-03-16
申请号：EP89203194.9
申请日：1989-12-14
申请人： SCLAVO S.p.A.
发明人： Pinori, Massimo , Centini, Felice , Verdini, Antonio Silvio
IPC分类号： C07K1/02 , C07K1/12 , C07K5/02 , C07D319/06
CPC分类号： C07K1/02 , C07D319/06 , C07K5/0212

3. 发明公开

EP0375040A3 Process for the preparation of retro-inverso peptides and new intermediates thereof 失效
标题翻译：制备逆转录酶的方法及其新的中间体
公开(公告)号：EP0375040A3
公开(公告)日：1991-07-03
申请号：EP89203194.9
申请日：1989-12-14
申请人： SCLAVO S.p.A.
发明人： Pinori, Massimo , Centini, Felice , Verdini, Antonio Silvio
IPC分类号： C07K1/02 , C07K1/12 , C07K5/02 , C07D319/06
CPC分类号： C07K1/02 , C07D319/06 , C07K5/0212
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.

4. 发明公开

EP0375040A2 Process for the preparation of retro-inverso peptides and new intermediates thereof 失效
标题翻译： Verfahren zur Herstellung von Retro-Inverso-Peptiden und dessen Zwischenprodukte。
公开(公告)号：EP0375040A2
公开(公告)日：1990-06-27
申请号：EP89203194.9
申请日：1989-12-14
申请人： SCLAVO S.p.A.
发明人： Pinori, Massimo , Centini, Felice , Verdini, Antonio Silvio
IPC分类号： C07K1/02 , C07K1/12 , C07K5/02 , C07D319/06
CPC分类号： C07K1/02 , C07D319/06 , C07K5/0212
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.
摘要翻译：一种合成部分逆转肽的方法，其包含至少一种式（III）-CO-H-CO-（III）的丙二酰残基，其中R表示α-氨基酸的侧链，其是其特征在于所述丙二酰残基通过将式（VI）的5-取代-2,2-二甲基-1,3-二恶烷-4,6-二酮缩合成CHEM，其中R min是侧链R，其中如果有的话，官能团被适当地保护，其中氨基酸，氨基酰胺，肽片段或假肽片段，其中如果存在末端羧基，并且可能的侧链官能团被适当地保护，并且反应性氨基是三烷基甲硅烷基化的。还描述和要求保护新的式（VI）化合物和涉及使用所述方法和所述中间体的部分逆转型绒毛蛋白类似物的制备方法。

5. 发明公开

EP0152977A1 Process for the preparation of L-alpha-aminoacids 失效
标题翻译： Verfahren zur Herstellung von L-alpha-Aminosäuren。
公开(公告)号：EP0152977A1
公开(公告)日：1985-08-28
申请号：EP85200098.3
申请日：1985-01-31
申请人： SCLAVO S.p.A.
发明人： Olivieri, Roberto , Eletti Bianchi, Giancarlo , Fascetti, Eugenio , Centini, Felice
IPC分类号： C12P13/04 , C12P13/06 , C12P13/22 , C12P13/08 , C07C101/02 , C07C101/08
CPC分类号： C12P41/009 , C12P17/10
摘要： Process for the preparation of L-a-aminoacids
wherein R is an aromatic, substituted aromatic, aliphatic or substituted aliphatic group, in which process:

a) An N-carbamyl-a-aminoacid compound of formula:
vherein R has the above-specified meaning and in the form of D-N-carbamyl-α-aminoacid and L-N-carbamyl-a-aminoacid is con- acted, in a liquid reaction mixture, and at a pH of from 6,0 to 7,0 and at a temperature of from 20°C to 40°C, with an enzyme to give a compound of formula
wherein R has the above-specified meaning, in the form of D-hydantoin, and a compound of formula
wherein R has the above-indicated meaning, in the form of L-N-carbamyl-a-aminoacid;
b) D-hydantoin is separated from the reaction mixture, and is hydrolyzed and racemized to D-N-carbamyl-a-aminoacid, and L-N-carbamyl-a-aminoacid;
c) L-N-carbamyl-a-aminoacid is trasformed into corresponding L-a-aminoacid;
d) L-a-aminoacid is separated and recovered from the reaction mixture.
摘要翻译：制备L-α-氨基酸的方法... 其中R是芳族取代的芳族，脂族或取代的脂族基团，其中方法：a）N-氨基甲酰-α-氨基酸化合物，其结构如下：其中R具有上述含义并以DN-氨基甲酰-α-氨基酸的形式，并且在氨基甲酰基-α-氨基酸中的液体反应混合物中，并且pH为6.0 在20℃至40℃的温度下加酶，得到式...的化合物 ...其中R具有D-乙内酰脲形式的上述含义，和其中R具有上述含义，以LN-氨基甲酰-α-氨基酸的形式; b）D-乙内酰脲与反应混合物分离，并水解并外消旋化为DN - 氨基甲酰-α-氨基酸和LN-氨基甲酰-α-氨基酸; c）将LN-氨基甲酰-α-氨基酸转变成相应的L-氨基酸无酸; d）从反应混合物中分离并回收L-α-氨基酸。

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