专利号:US-9920084-B2 优先权日:2011-08-23 标题 :Ionic tags for synthesis of oligoribonucleotides 发明人:DAMHA MASAD J; HASSLER MATTHEW; CHAN TAK-HANG; NANDYALA MALLIKARJUNA REDDY; DONGA ROBERT ALEXANDER 权利人:DAMHA MASAD J; HASSLER MATTHEW; CHAN TAK HANG; NANDYALA MALLIKARJUNA REDDY; DONGA ROBERT ALEXANDER; THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIV; HONG KONG POLYTECHNIC UNIV 摘要:The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II) processes for making these compounds, and the use thereof in the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. The invention also relates to methods of synthesis of oligomers, including but not limited to oligopeptides, oligosaccharides and oligonucleotides, particularly oligoribonucleotides and also oligodeoxyribonucleotides, in solution systems, and ionic tag linkers for use in methods provided herein.
专利号:WO-9002605-A1 优先权日:1988-09-02 标题:An apparatus and a method for the synthesis of peptides 发明人:MELDAL MORTEN; HOLM ARNE; BUCHARDT OLE 权利人:MELDAL MORTEN; HOLM ARNE; BUCHARDT OLE 摘要:An apparatus for use in chemical synthesis, especially peptide synthesis, comprises a synthesis chamber unit having a multiplicity of synthesis chambers, each of which has a liquid inlet and a liquid outlet, means for introducing liquid into the individual synthesis chambers and means for simultaneous removal of liquid via the liquid outlets of the synthesis chambers by regulation of the fluid pressure difference between the liquid inlets and the liquid outlets. A method for peptide synthesis using such an apparatus comprises the provision in each of the synthesis chambers of a solid-phase support material having a first, at least N-protected amino acid coupled thereto, after which a liquid deprotection reagent is introduced into the synthesis chambers. Following deprotection, the deprotection reagent is removed, after which a second, at least N-protected amino acid is introduced into each synthesis chamber in order to couple the first and second amino acids. Third, fourth, etc. amino acids may be coupled analogously. Complete removal of the deprotection reagent from the synthesis chambers and the support material can be ensured by incorporating a stable, intensely coloured dye, e.g., azorubin, in the deprotection reagent. The apparatus and the method make possible the parallel synthesis of a large number of peptides, e.g. peptides having overlapping amino acid sequences and constituting part of a longer peptide chain. The apparatus can be adapted to manual, semi-automatic or fully automatic performance of the various steps in the synthesis procedure.
专利号:US-2019292219-A1 优先权日:2018-03-26 标 题:Method of solid-state peptide synthesis using a novel polymeric support 发明人:JERABEK KAREL; HANKOVA LIBUSE; HOLUB LADISLAV; ZECCA MARCO; CENTOMO PAOLO; TROVO DANIELE; LEDER RICCARDO; BIONDI BARBARA 权利人:INST OF CHEMICAL PROCESS FUNDAMENTALS OF THE CAS V V I; UNIV DEGLI STUDI PADOVA 摘要:A method of solid-state synthesis of peptides that provides a polymeric solid-state synthesis support, attaches a first amino acid to said support to form the first amino acid molecule of the desired peptide chain, attaches additional amino acids to form the desired peptide chain, characterized in that the polymeric solid-state synthesis support is a styrenic polymer containing at least 50 mol % divinylbenzene monomer units, the styrenic polymer being functionalized with chloromethyl and/or benzyloxybenzyl alcohol and/or amino moieties, and having porosity 60-90% and medium pore diameter ranging from 10 to 80 nm. A functionalized styrenic polymer is claimed.
专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-11466050-B2 优先权日:2014-09-29 标 题 :Method for peptide synthesis and apparatus for carrying out a method for solid phase synthesis of peptides 发明人:KNAUER SASCHA; ROESE TOBIAS MICHAEL LOUIS; AVRUTINA OLGA; KOLMAR HARALD; UTH CHRISTINA 权利人:SULFOTOOLS GMBH 摘要:The invention relates to a method for peptide synthesis, wherein said method comprises the steps of reacting a first amino acid or a first peptide with an α-amine protected second amino acid in a solvent selected from the group consisting of water, alcohol, and a mixture of water and alcohol, and removing the α-amine protecting group with a deprotecting solution. The invention further relates to protective agents, their use and an apparatus for carrying out a method for solid phase synthesis of peptides.
专利号:US-5977301-A 优先权日:1992-09-24 标题 :Synthesis of N-substituted oligomers 发明人:ZUCKERMAN RONALD N; KERR JANICE M; KENT STEPHEN B H; MOOS WALTER H; SIMON REYNA J; GOFF DANE A 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
[参考文献]: Adam J Mcshane, Et Al. Peptide Dimethylation: Fragmentation Control Via Distancing The Dimethylamino Group. J Am Soc Mass Spectrom. 2014 Oct;25(10):1694-704. [参考文献]: Basavaraj Siddalingappa, Et Al. Stabilization Of Resveratrol In Blood Circulation By Conjugation To Mpeg And Mpeg-Pla Polymers: Investigation Of Conjugate Linker And Polymer Composition On Stability, Metabolism, Antioxidant Activity And Pharmacokinetic Profile. Plos One. 2015 Mar 23;10(3):E0118824. [参考文献]: Egan J Lohman#, Et Al. Optimized Inorganic Carbon Regime For Enhanced Growth And Lipid Accumulation In Chlorella Vulgaris. Biotechnol Biofuels. 2015 Jun 11:8:82. [参考文献]: Francisca C Moreira, Et Al. Incorporation Of Electrochemical Advanced Oxidation Processes In A Multistage Treatment System For Sanitary Landfill Leachate. Water Res. 2015 Sep 15:81:375-87. [参考文献]: Lucas A Lane, Et Al. Compact And Blinking-Suppressed Quantum Dots For Single-Particle Tracking In Live Cells. J Phys Chem B. 2014 Dec 11;118(49):14140-7.
合成参考文献
参考文献:10.1155/2011/254095 摘要:Shi L, Fleming CJ, Riechers SL, Yin N, Luo J, Lam KS, Liu G. High-Resolution Imaging of Dendrimers Used in Drug Delivery via Scanning Probe Microscopy. Journal of Drug Delivery. 2011 Jun 13;2011():1–12. doi: 10.1155/2011/254095.