三乙二醇置于2,2,6,6-Tetramethyl-Piperidine-N-Oxyl,碳酸氢钠,Sodium Carbonate体系中,用94%的收率获得3,6-二氧苯贰酸 参考文献:Electroorganic Synthesis In Oil-In-Water Nanoemulsion: Tempo-Mediated Electrooxidation Of Amphiphilic Alcohols In Water 标题:Electroorganic Synthesis In Oil-In-Water Nanoemulsion: Tempo-Mediated Electrooxidation Of Amphiphilic Alcohols In Water 摘要:水包油纳米乳液,由tempo,两亲性醇和水组成,为醇的电氧化提供了独特的反应环境,从而以非常好至优异的收率获得了相应的羧酸. Doi:10.1055/s-2007-991070
专利号:US-10526379-B2 优先权日:2015-06-05 标题:Methods and products for fusion protein synthesis 发明人:HOWARTH MARK 权利人:UNIV OXFORD INNOVATION LTD 摘要:A method of producing a fusion protein is provided. The method includes: a) contacting a first protein with a second protein under conditions that enable the formation of an isopeptide bond between said proteins to form a linked protein; and b) contacting the linked protein from (a) with a third protein under conditions that enable the formation of an isopeptide bond between said third protein and said linked protein to form a fusion protein. Peptide linkers and the use of orthogonal pairs of said linkers in the synthesis of fusion proteins are also provided. Recombinant proteins comprising said linkers, nucleic acid molecules encoding said proteins and linkers, vectors comprising said nucleic acid molecules and host cells comprising said vectors and nucleic acid molecules are also contemplated.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:US-5922840-A 优先权日:1996-07-23 标 题 :Methods for purifying synthetic peptides 发明人:TOMICH JOHN M; IWAMOTO TAKEO 权利人:UNIV KANSAS STATE 摘要:Methods for making preparations of homogenous peptides are disclosed. In these methods, reversible alterations of the physicochemical properties of the peptides are exploited. In preferred embodiments, the methods include the following sequential steps: (1) exhaustive capping is carried out during solid-phase synthesis of a desired peptide; (2) a cleavable linker is attached to the peptide, (3) a polymer is added to the peptide either by condensation with preformed polymer or by in situ polymerization such that the linker is interposed between the polymer moiety and the peptide moiety of the resultant adduct; alternatively, steps (2) and (3) can be conducted simultaneously by attaching a combination polymer/linker to the peptide; (4) the polymer-peptide adduct is cleaved from the resin; (5) the polymer-peptide adduct is purified from undesired, nonadducted peptides; and (6) the polymer-peptide adduct is cleaved at the linker, and the desired peptide is purified from the polymer. In some cases, it may be desirable to omit step (6) in order to leave the polymer moiety attached to the desired peptide. For example, the polymer-peptide adducts of the present invention are very soluble in water, and therefore can be used to solubilize amphipathic peptides. Additionally, the polymer moieties of the polymer-peptide adducts can elicit immune responses in mammals or birds; thus, the adducts and corresponding antibodies can be used in research protocols to track the peptide moieties of the adducts.
专利号:ES-2880336-T3 优先权日:2015-06-05 标题:Methods and products for the synthesis of fusion proteins
专利号:TW-200914433-A 优先权日:2007-07-03 标 题:Process and intermediates for the synthesis of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds
专利号:US-7179794-B2 优先权日:1998-06-08 标题 :Multivalent macrolide antibiotics 发明人:GRIFFIN JOHN H; PACE JOHN L 权利人:THERAVANCE INC 摘要:Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptoramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.
1: Bonache MA, Alaimo A, Malo C, Millet O, Villarroel A, González-Muñiz R. Clicked bis-PEG-peptide conjugates for studying calmodulin-Kv7.2 channel binding. Org Biomol Chem. 2014 Nov 28;12(44):8877-87. doi: 10.1039/c4ob01338g. doi: 10.1021/ol500363r. Epub 2014 Mar 7. doi: 10.1111/j.1747-0285.2012.01394.x. Epub 2012 May 30.
合成参考文献
摘要:G. Ostacoli, E. Campi, N. Cabrario and G. Saini, Gazz. Chim. Ital. 91, 349 (1961).