专利号:US-2004038331-A1 优先权日:2002-08-23 标题:Solid phase synthesis of biomolecule conjugates 发明人:REDDY M PARAMESWARA; FAROOQUI FIRDOUS; BRILLHART KURT L 摘要:Processes for the solid state phase formation synthesis of biomolecule conjugates, particularly protein-oligonucleotide conjugates are shown. One of the protein or oligonucleotide is reversibly bound to a solid substrate phase. At least one portion of each of the protein and the oligonucleotide molecules is activated with complementary activation groups. The activated protein and the activated oligonucleotide are then reacted, in a buffered solution resulting in the formation of the desired conjugate which remains reversibly bound to the substrate. The nature of the buffered solution is then modified causing the conjugate to be released from the substrate solid phase.
专利号:US-6919382-B2 优先权日:2000-08-31 标 题 :Preparation and uses of conjugated solid supports for boronic acids 发明人:HALL DENNIS G 权利人:UNIV ALBERTA 摘要:The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.
专利号:US-2023212216-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins 发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH 权利人:GENIE BIOTECH UK LTD 摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.
专利号:EP-1314727-B1 优先权日:2001-11-23 标题 :Direct synthesis of quaternary phenanthridinium salts 发明人:CAPELLE NICOLAS; GALLO ROGER 权利人:MERIAL SAS 摘要:Process for the preparation of phenanthridinium quaternary salts (I) comprises reacting a halo-aromatic compound (II) with a phenyl boronic derivative (III) in a basic medium, in the presence of a palladium catalyst. ?>Process for the preparation of phenanthridinium quaternary salts of formula (I) comprises reacting a halo-aromatic compound of formula (II) with a phenyl boronic derivative of formula (III) in a basic medium, in the presence of a palladium catalyst. ?>R<3>, R<8> = an electro-attractor group having an electronegativity at last equal to that of nitro; ?>R<5> = a non-chemically labile group; ?>R<6> = aryl or 5-12C heteroaryl, which my be condensed and may have one or more hetero atoms; ?>X<-> = a halide or hydrogen sulfate anion or a base joined to a mineral acid; ?>X = halogen; ?>R = H; ?>R+R = a group of formula (i); ?>n, n' = 0-4; ?>R<9>, R<10> = H or 1-5C alkyl. ?>Independent claims are also included for: ?>(1) intermediates of formula (VI); and ?>(2) the preparation of (VI). ?>X1 = halogen.
专利号:WO-0112791-A1 优先权日:1999-08-12 标 题 :Dna shuffling of dioxygenase genes for production of industrial chemicals 发明人:SELIFONOV SERGEY A; NEWMAN LISA M 权利人:MAXYGEN INC; SELIFONOV SERGEY A; NEWMAN LISA M 摘要:This invention provides improved polypeptides, including dioxygenases, dehydrogenases, ligases and transferases that are useful for the biocatalytic synthesis of compounds such as α-hydroxycarboxylic acids, and aryl- and alkyl-hydroxy and carboxylic acid compounds. The polypeptides provided herein are improved in properties such as regioselectivity, enzymatic activity, stereospecificity, and the like. Methods for obtaining recombinant polynucleotides that encode these improved polypeptides are also provided, as are organisms that express the polypeptides and are thus useful for carrying out said biocatalytic syntheses. Also provided by the invention are methods for increasing said solvent resistance of organisms that are used in the synthetic methods.
专利号:US-6605430-B1 优先权日:1998-08-12 标题 :DNA shuffling of monooxygenase genes for production of industrial chemicals 发明人:AFFHOLTER JOSEPH A; DAVIS S CHRISTOPHER; SELIFONOV SERGEY A 权利人:MAXYGEN INC 摘要:This invention provides improved monoxygenases, dehydrogenases, and transferases that are useful for the biocatalytic synthesis of compounds such as α-hydroxycarboxylic acids, and aryl- and alkyl-hydroxy compounds. The polypeptides provided herein are improved in properties such as regioselectivity, enzymatic activity, stereospecificity, and the like. Methods for obtaining recombinant polynucleotides that encode these improved polypeptides are also provided, as are organisms that express the polypeptides and are thus useful for carrying out said biocatalytic syntheses. Also provided by the invention are methods for increasing said solvent resistance of organisms that are used in the synthetic methods.
摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 203. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 116. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 199. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 22.