专利号:WO-2010103857-A1 优先权日:2009-03-12 标 题 :Method for solid-phase synthesis of glycopeptide using silicon-containing protecting group and synthesis device 发明人:NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN 权利人:UNIV HOKKAIDO NAT UNIV CORP; NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN 摘要:Disclosed are a novel method for the synthesis of a glycopeptide by which glycopeptides of various types can be deprotected and excised from a resin, each under weakly acidic to weakly basic conditions, without causing the problems of the epimerization of an amino acid at the a-position and the ß-elimination of a sugar residue; a synthesis device therefor; and a synthesis intermediate to be used in synthesizing a glycopeptide. Specifically disclosed are a method for the solid-phase synthesis of a glycopeptide which comprises a step for obtaining a glycopeptide derivative wherein the N-terminus is protected, the C-terminus is immobilized to a solid phase via a silicon linker, and a reactive group carried by a sugar residue and a reactive group carried by an amino acid side chain constituting a peptide are protected by silicon-containing groups, and a step for obtaining the glycopeptide by deprotecting said glycopeptide derivative and releasing the same from the solid phase by treating the glycopeptide derivative with an agent for removing the silicon-containing groups and the silicon linker; a synthesis intermediate to be used in the step for obtaining the glycopeptide derivative in the aforesaid method; and a device for the solid-phase synthesis of a glycopeptide.
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-6696590-B2 优先权日:2000-12-22 标题 :Process for the synthesis of aliphatic, cycloaliphatic or araliphatic chloroformates 发明人:BONNARD HUBERT; FERRUCCIO LAURENCE; GAUTHIER PATRICIA; SENET JEAN-PIERRE 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The disclosure relates to a process for the synthesis of substituted or unsubstituted aliphatic, cycloaliphatic or araliphatic chloroformates by reaction of the corresponding alcohol with phosgene, diphosgene and/or triphosgene. The reaction is carried out under a pressure of between 15×10 3 Pa and 85×10 3 Pa and at a temperature of between −30° C. and +50° C. The process is particularly well suited to the preparation of menthyl chloroformate and benzyl chloroformate.
专利号:US-4504415-A 优先权日:1983-04-04 标题:Synthesis of thymosin α1 and desacetyl thymosin α1 发明人:FELIX ARTHUR M; GILLESSEN DIETER; STUDER ROLF; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD 权利人:HOFFMANN LA ROCHE 摘要:An improved solution phase synthesis of thymosin alpha 1 and desacetyl thymosin alpha 1 with t-Boc side chain protection and proceeding through novel intermediates is disclosed.
专利号:US-4517119-A 优先权日:1983-04-04 标题:Synthesis of thymosin α1 发明人:FELIX ARTHUR M; GILLESSEN DIETER; LERGIER WILLIAM; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD 权利人:HOFFMANN LA ROCHE 摘要:An improved solution phase synthesis of thymosin α 1 and proceeding through novel intermediates is disclosed.
专利号:WO-0037486-A1 优先权日:1998-12-22 标题:Synthesis and recovery of aspartame involving enzymatic deformylation step 发明人:QUAEDFLIEG PETER JAN LEONARD M; SONKE THEODORUS; WAGNER ADOLF FRITZ VOLKER 权利人:HOLLAND SWEETENER CO; QUAEDFLIEG PETER JAN LEONARD M; SONKE THEODORUS; WAGNER ADOLF FRITZ VOLKER 摘要:The invention relates to the synthesis of aspartame involving enzymatic deformylation of an N-formyl-α-L-aspartyl-L-phenylalanine compound by treatment with an enzyme having formylmethionyl peptide deformylase activity and having as a co-factor group 5 to 11 bivalent metal ions. The invention also relates to selective preparation and recovery of aspartame from a mixture of N-formyl-α- and β-L-aspartyl-L-phenylalanine compounds by treatment with such enzyme. And finally, the invention relates to one-pot enzymatic synthesis of aspartame from N-formyl-L-aspartic acid and L- or D,L-phenylalanine methyl ester involving an enzymatic deformylation reaction simultaneously with an enzymatic coupling reaction, as well as to one-pot di- or oligopeptide synthesis by simultaneous enzymatic coupling and deformylation reactions in general.
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
摘要:Servi, S.; Tessaro, D.; Hollmann, F., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 15.