专利号:WO-2025044766-A1 优先权日:2023-08-31 标题:Use of silicon dioxide microspheres in synthesis of ultra-long oligonucleotide and method for synthesizing ultra-long oligonucleotide 发明人:SHI YONGYONG; ZHANG MANCANG; WANG LIBING; GAO PANPAN; FANG JUN 权利人:UNIV SHANGHAI JIAOTONG; SHANGHAI DYNEGENE TECH CO LTD 摘要:The present invention relates to the technical field of oligonucleotide synthesis. Disclosed are the use of silicon dioxide microspheres in the synthesis of an ultra-long oligonucleotide and a method for synthesizing an ultra-long oligonucleotide, wherein the silicon dioxide microspheres have a specific surface area of less than 1 m2/g, and preferably, the silicon dioxide microspheres have modification groups on the surface. The method for synthesizing an ultra-long oligonucleotide comprises: performing a coupling reaction on a nucleoside phosphoramidite synthesis unit using the silicon dioxide microspheres having modification groups on the surface as carriers under coupling reaction conditions. The prepared carriers can be used to prepare an ultra-long oligonucleotide.
专利号:US-7781488-B2 优先权日:2002-06-10 标 题:Post-cleavage sulfur deprotection for convergent protein synthesis by chemical ligation 发明人:BOTTI PAOLO; VILLAIN MATTEO; MANGANIELLO SONIA; GAERTNER HUBERT 权利人:AMYLIN PHARMACEUTICALS INC 摘要:The present invention provides a method and compositions for synthesizing an oligopeptide or polypeptide by convergent assembly of a plurality of pairs of oligopeptides in chemical ligation reactions. An important aspect of the present invention is an oligopeptide having a C-terminal disulfide-protected carboxythioester group that can be deprotected to spontaneously generate a free C-terminal thioester moiety. This allows a single precursor to participate in a succession of chemical ligation reactions, thereby making the convergent synthesis approach possible. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins, and improves the efficiency of native chemical ligation reactions, particularly where four or more peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
专利号:US-12337036-B2 优先权日:2018-01-01 标题:Compounds and methods for trans-membrane delivery of molecules 发明人:ZIV ILAN; GRIMBERG HAGIT; DUBROVSKY JOSEPH 权利人:APOSENSE LTD 摘要:The Invention provides a novel delivery system for delivery of drugs across biological membranes. It provides novel chemical conjugates that comprise said delivery system, methods for synthesis of said compounds, and methods for utilization of said delivery system, among others, for delivery of genetic drugs into tissues and cells, in vitro, ex vivo, and in vivo, for the treatment of various medical disorders.
专利号:US-8012448-B2 优先权日:2009-07-13 标题 :Synthesis of metal chalcogenide nanocrystals using organodichalcogenide reagents 发明人:BRUTCHEY RICHARD L; FRANZMAN MATTHEW A; WEBBER DAVID H 权利人:UNIV SOUTHERN CALIFORNIA 摘要:A method of synthesizing metal chalcogenide nanocrystals involving the steps of combining an organodichalcogenide, a metal salt and a ligand compound to form a mixture; degassing the mixture to remove air and water from the mixture; heating the mixture at a temperature below the decomposition temperature of the organodichalcogenide for a period of time sufficient to form a metal chalcogenide nanocrystal.
专利号:US-6573387-B1 优先权日:1997-03-21 标 题 :Synthesis of α,β-substituted amino amides, esters, and acids 发明人:SHARPLESS K BARRY; RUBIN A ERIK 权利人:SCRIPPS RESEARCH INST 摘要:α,β-Unsaturated amides and esters are converted to α,β-substituted amino amides, esters, and acids. An α,βunsaturated amide or ester is first converted to an α,β-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The α,β-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a α,β-N-sulfonyl- or the α,β-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(α,β-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.
专利号:US-9090629-B2 优先权日:2010-11-03 标题:Cytotoxic agents comprising new ansamitocin derivatives 发明人:CHARI RAVI V J; WIDDISON WAYNE C; WILHELM SHARON D 权利人:CHARI RAVI V J; WIDDISON WAYNE C; WILHELM SHARON D; IMMUNOGEN INC 摘要:New ansamitocin derivatives bearing a linking group are disclosed. Also disclosed are methods for the synthesis of these new ansamitocin derivatives and methods for their linkage to cell-binding agents. The ansamitocin derivative-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.
[参考文献]: Suzanne A Blum, Et Al. Enantioselective Oxidation Of Di-Tert-Butyl Disulfide With A Vanadium Catalyst: Progress Toward Mechanism Elucidation. J Org Chem. 2003 Jan 10;68(1):150-5.
合成参考文献
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