专利号:US-7435791-B2 优先权日:2001-07-19 标题:Process for rapid solution synthesis of peptides 发明人:EGGEN IVO FRANCI; TEN KORTENAAR PAULUS BERNARDUS; HAASNOOT CORNELIS ALBERT GRUSON 权利人:ORGANON NV 摘要:The present invention relates to a process for rapid solution synthesis of a peptide, the process comprising repetitive cycles of steps (a)-(d):n (a) a coupling step, using an excess of an activated carboxylic component to acylate an amino component, (b) a quenching step in which a scavenger is used to remove residual activated carboxylic functions, wherein the scavenger may also be used for deprotection of the growing peptide, (c) one or more aqueous extractions and optionally, (d) a separate deprotection step, followed by one or more aqueous extractions, characterised in that the process comprises at least one step (b), referred to as step (b′), in which an amine or a thiol comprising a free anion or a latent anion is used as a scavenger of residual activated carboxylic functions. nn During the process of this invention the growing peptide need not be isolated until the final peptide sequence has been obtained. n This highly efficient process is useful for the production of oligo- and polypeptides of high purity.
专利号:US-10961273-B2 优先权日:2016-08-16 标 题 :N-carboxyanhydride-based-scale synthesis of elamipretide 发明人:DUNCAN SCOTT M; OUDENES JAN; ANDERSEN MARC W 权利人:STEALTH BIOTHERAPEUTICS CORP 摘要:Disclosed are methods of making elamipretide (MTP-131), a peptide compound with therapeutic potential for treating various mitochondrial myopathies. The synthesis of the peptide can be achieved via the use of N-carboxyanhydride-modified amino acid residues, which increases the efficiency of the synthetic process and the purity of the peptide product generated.
专利号:US-4914214-A 优先权日:1987-09-17 标 题:Process for the industrial synthesis of perindopril 发明人:VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES 权利人:ADIR 摘要:Process for the industrial synthesis of perindopril, in which (2S,3aS,7aS)-2-carboxyperhydroindole is condensed with N-[(S)-1-carbethoxybutyl]-(S)-alanine after protection of the carboxyl group, the product resulting from the condensation being then subjected to deprotection of the carboxyl carried by the heterocyclic ring. n The (2S,3aS,7aS)-2-carboxyperhydroindole and N-[(S)-1-carbethoxybutyl]-(S)-alanine are themselves obtained in excellent conditions from 2-carboxyindole and from L-alanine respectively, both available on an industrial scale.
专利号:EP-2607373-A1 优先权日:2011-12-23 标 题 :Liquid phase synthesis of self-assembling peptides to be linked to polymers or to other bioactive and/or self-assembling peptides 发明人:MOUSSA WAFA; JEANNIN LAURENT; CALLENS ROLAND; BOUSMANNE MARTIN 权利人:SOLVAY 摘要:The present invention relates to a process for preparing a peptide moiety comprising an amino acid sequence (I) n€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ R-Xaa1-Xaa5-Xaa3-Xaa6-R1€ƒ€ƒ€ƒ€ƒ€ƒ(I), nwherein R1 is selected from OH and NH 2 nand a peptide moiety comprising an amino acid sequence (II) n€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ H-Xaa1-Xaa2-Xaa3-Xaa4-Xaal-Xaa5-Xaa3-Xaa6-R1€ƒ€ƒ€ƒ€ƒ€ƒ(II), nwherein R1 is selected from OH and NH 2 nwhereby Xaa1 and Xaa3 are residues of hydrophobic amino acids and are preferably selected from the group consisting of phenylalanine, tryptophan, histidine, tyrosine, isoleucine, alanine, leucine, norleucine and valine ; and Xaa2, Xaa4, Xaa5 and Xaa6 are residues of charged amino acids and are preferably selected from the group consisting of arginine, aspartic acid, glutamic acid and lysine. The invention further relates to a process for synthesis of a polymer covalently linked with at least one peptide, wherein the peptide comprises said peptide moiety.
专利号:US-7157484-B2 优先权日:2003-02-28 标 题 :Method for synthesissing (2s, 3as, 7as)-perhydroindole-2-carboxylic acid and the esters thereof and the use thereof for perindopril synthesis 发明人:DUBUFFET THIERRY; LANGLOIS PASCAL 权利人:SERVIER LAB 摘要:Process for the synthesis of compounds of formula (I): n nwherein R represents hydrogen or a protecting group.n n Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
专利号:WO-2010077155-A1 优先权日:2008-12-31 标 题 :A method of producing an n-blocked peptide 发明人:LIPKOWSKI ANDRZEJ 权利人:ACTION FOR DEV OF RES SP Z O O; LIPKOWSKI ANDRZEJ 摘要:The perspective uses of using peptides as drags require economical synthesis methods. It was shown that N-blocked peptide derivatives constituting the raw material for use in peptide synthesis may be obtained through the modification of the synthesis, which is based on the acylation of an appropriate organic amino-acid salt using an appropriate active derivative of an amino-acid or peptide.
1: Carter DB, Chae CB. Chromatin-bound protease: degradation of chromosomal proteins under chromatin dissociation conditions. Biochemistry. 1976 Jan 13;15(1):180-5. doi: 10.1016/j.bbapap.2011.10.007. Epub 2011 Oct 19. doi: 10.1016/j.ejmech.2008.07.017. Epub 2008 Jul 23.
合成参考文献
摘要:Zhou, Q.-Q.; Wei, Y.; Lu, L.-Q.; Xiao, W.-J., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 204. 摘要:Primer, D. N.; Molander, G. A., Science of Synthesis, (2019) , 324.