专利号:US-2024218014-A1 优先权日:2022-11-21 标 题:Synthesis of a cyclic peptide 发明人:BAUR PIUS BRUNO; CLEATOR EDWARD; DENIAU GILDAS; EISELE FRANK; FLÖGEL OLIVER; HUSTE ANJA; KEHL MARCEL ROMAN; LÖWENECK MARKUS; SILVA ROLANDO RAVELO; VORBERG RAFFAEL 权利人:JANSSEN PHARMACEUTICA NV 摘要:Processes for performing peptide synthesis, particularly for cyclic peptide synthesis are generally described. Reaction intermediates of the peptide synthesis are also described.
专利号:US-5455363-A 优先权日:1991-10-11 标题 :Amino acid derivatives for peptide synthesis 发明人:GOSTELI JACQUES; SAX BEAT; DICK FRITZ; TANNER RUDOLF 摘要:Compounds of formula I are described, I wherein n is equal to one or two, R1 stands for hydrogen or an amino protecting group, R2 represents hydrogen or a carboxyl protecting group and R3 4-methyltriphenylmethyl, 4,4'-dimethyltriphenylmethyl, 4,4',4''-trimethyltriphenylmethyl. Furthermore described are compounds of formula I which are reactive and suitable for coupling reactions and are derived from I with R2=H by activation of the carboxyl group. The compounds mentioned above can be used as starting materials for the synthesis of peptides. They are more suitable than analogous compounds of formula I, wherein R3 represents hydrogen or a carbamoyl protecting group used hitherto.
专利号:US-2003153783-A1 优先权日:1999-06-30 标题:Synthesis of (R) and (S)-aminocarnitine, (R) and (S)-4-phosphonium-3-amino-butanoate, (R) and (S) 3,4-diaminobutanoic acid, and their derivatives starting from D- and L-aspartic acid 发明人:GIANNESSI FABIO; DELL UOMO NATALINA; TINTI MARIA ORNELLA; DE ANGELIS FRANCESCO 权利人:SIGMA TAU IND FARMACEUTI 摘要:A process is described for the preparation of R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives with the following formula: n n n where Y is as described in the attached description, starting from aspartic acid with the same configuration as the desired compounds. This process is advantageous from the industrial point of view in terms of the type of reactants used, the reduced volumes of solvents and the possibility of avoiding purification of the intermediate products.
专利号:US-6822115-B2 优先权日:1999-06-30 标 题:Synthesis of (R) and (S)-aminocarnitine, (R) and (S)-4-phosphonium-3-amino-butanoate, (R) and (S) 3,4-diaminobutanoic acid, and their derivatives starting from D- and L-aspartic acid 发明人:GIANNESSI FABIO; DELL UOMO NATALINA; TINTI MARIA ORNELLA; DE ANGELIS FRANCESCO 权利人:SIGMA TAU IND FARMACEUTI 摘要:R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives are prepared using n starting from aspartic acid with the same configuration as the desired compounds. This process is advantageous from the industrial point of view in terms of the type of reactants used, the reduced volumes of solvents and the possibility of avoiding purification of the intermediate products.
专利号:US-6528684-B1 优先权日:1999-06-30 标题 :Synthesis of (R) and (S) -aminocarnitine and their derivatives starting from D- and L-aspartic acid 发明人:GIANNESSI FABIO; DELL UOMO NATALINA; TINTI MARIA ORNELLA; DE ANGELIS FRANCESCO 权利人:SIGMA TAU IND FARMACEUTI 摘要:R or S aminocarnitine and their derivatives with formula (I)where Y is as described in the description, starting with aspartic acid with the same configuration as the aminocarnitine desired. This process has advantage in the type of reactants used, reduced volumes of solvents and the possibility of avoiding purification of intermediate products.
专利号:US-3725380-A 优先权日:1969-04-05 标 题:Method of synthesizing peptides in the presence of a carbodiimide and a 1-hydroxy-benzotriazole 发明人:KONIG W; GEIGER R 权利人:HOECHST AG 摘要:Improved synthesis of peptides by the carbodiimide method in which an amino-protected amino acid or peptide having a reactive carboxy group is condensed with a carboxy-protected amino acid or peptide having a reactive amino group in the presence of a 1hydroxy-benzotriazole or a substituted 1-hydroxy-benzotriazole of the formula AS WELL AS IN THE PRESENCE OF A CARBODIIMIDE SUCH AS DICYCLOHEXYL CARBODIIMIDE.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1016/j.bbrc.2023.08.050 摘要:Ikeda Y, Davis MI, Sumita K, Zheng Y, Kofuji S, Sasaki M, Hirota Y, Pragani R, Shen M, Boxer MB, Takeuchi K, Senda T, Simeonov A, Sasaki AT. Multimodal action of KRP203 on phosphoinositide kinases in vitro and in cells. Biochemical and Biophysical Research Communications. 2023 Oct;679():116–21. doi: 10.1016/j.bbrc.2023.08.050.