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-11414375-B2 优先权日:2016-07-29 标题:Mild and efficient preparation method for α-acyloxyenamide compounds and use thereof in synthesis of amide and polypeptide 发明人:ZHAO JUNFENG; HU LONG; XU SILIN; ZHAO ZHENGUANG 权利人:UNIV JIANGXI NORMAL 摘要:Disclosed are a mild and efficient preparation method for an α-acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The α-acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0° C. to 50° C.; the produced α-acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.
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-2023220001-A1 优先权日:2020-06-09 标 题:Method for synthesis of thioether-containing peptides 发明人:GRUSS HENDRIK; LUTZ CHRISTIAN; SÜSSMUTH RODERICH; Yao guiyang; KNITTEL CAROLINE; KOSOL SIMONE; MAINZ ANDI 权利人:HEIDELBERG PHARMA RES GMBH 摘要:The present invention relates to a method of formation of a sulphur bridge between tryptophan and cysteine in solid phase peptide synthesis under iodine treatment. The invention also relates to the resulting compounds of the method and their respective use.
专利号:US-3953416-A 优先权日:1971-12-20 标 题:Synthetic decapeptide having the activity of the luteinizing hormone releasing hormone and method for manufacturing the same 发明人:FOLKERS KARL; CURRIE BRUCE L; CHANG JAW-KANG; SIEVERTSSON HANS; BOGENTOFT CONNY 权利人:FOLKERS KARL; CURRIE BRUCE L; CHANG JAW KANG; SIEVERTSSON HANS; BOGENTOFT CONNY 摘要:A synthetic decapeptide, L-pglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucy l-L-arginyl-L-prolyl-glycinamide which has the hormonal activities of the luteinizing hormone releasing hormone (LRH) of the hypothalamus gland of mammals is produced by utilizing as the key starting materials, the amino acids, glutamic acid or pyroglutamic acid, histidine, tryptophan, serine, tyrosine, glycine, leucine, arginine, and proline. Synthesis of the decapeptide is accomplished by coupling, in appropriate combinations of appropriate protected forms of the amino acids, and finally deprotecting to yield the amide, L-pglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucy l-L-arginyl-L-prolyl-glycinamide.
专利号:BR-PI0202783-B1 优先权日:2001-07-19 标 题:process for the rapid synthesis of a peptide in solution in an organic solvent or a mixture of organic solvents, and methods for the combinatorial synthesis of peptide collections and for automated solution peptide synthesis
参考标题:A Facile Synthesis Of Hydroxamic Acids OfNα-Protected Amino Acids Employing Bdms, A Study Of Their Molecular Docking And Their Antibacterial Activities 作者:K. Uma,H. S. Lalithamba,V. Chandramohan,K. Lingaraju |发布日期:2019.3.4 摘要:Hydroxamic Acids Have Received Much Attention As Biologically Active Compounds. Synthetic Hydroxamic Acids Enhance The Growth Of Plant Sources And Improve The Soil Quality, Act As Antibiotics, Cell...
合成参考文献
参考文献:10.1016/0006-8993(85)90764-4 摘要:Vigna SR, Szecòwka J, Williams JA. Do antagonists of pancreatic cholecystokinin receptors interact with central nervous system cholecystokinin receptors Brain Res. 1985 Sep 23;343(2):394–7. doi: 10.1016/0006-8993(85)90764-4.