专利号:US-12188072-B2 优先权日:2018-03-19 标题 :Compositions and methods for rapid in vitro synthesis of bioconjugate vaccines in vitro via production and N-glycosylation of protein carriers in detoxified prokaryotic cell lysates 发明人:JEWETT MICHAEL CHRISTOPHER; STARK JESSICA CAROL; DELISA MATTHEW P; JAROENTOMEECHAI THAPAKORN 权利人:UNIV NORTHWESTERN; UNIV CORNELL 摘要:Disclosed are methods, systems, components, and compositions for cell-free synthesis of glycosylated carrier proteins. The glycosylated carrier proteins may be utilized in vaccines, including anti-bacterial vaccines. The glycosylated carrier proteins may include a bacterial polysaccharide conjugated to a carrier, which may be utilized to generate an immune response in an immunized host against the polysaccharide conjugated to the carrier. The glycosylated carrier proteins may be synthesized in cell-free glycoprotein synthesis (CFGpS) systems using prokaryote cell lysates that are enriched in components for glycoprotein synthesis such as oligosaccharyltransferases (OSTs) and lipid-linked oligosaccharides (LLOs) including OSTs and LLOs associated with synthesis of bacterial O antigens.
专利号:US-12365930-B2 优先权日:2016-07-14 标题:Method for rapid in vitro synthesis of glycoproteins via recombinant production of N-glycosylated proteins in prokaryotic cell lysates 发明人:JEWETT MICHAEL CHRISTOPHER; STARK JESSICA CAROL; DELISA MATTHEW P; JAROENTOMEECHAI THAPAKORN 权利人:UNIV NORTHWESTERN; UNIV CORNELL 摘要:Disclosed are methods, systems, components, and compositions for cell-free synthesis of glycosylated proteins. The glycosylated proteins may be utilized in vaccines, including anti-bacterial vaccines. The glycosylated proteins may include a bacterial polysaccharide conjugated to a carrier, which may be utilized to generate an immune response in an immunized host against the polysaccharide conjugated to the carrier. The glycosylated proteins may be synthesized in cell-free glycoprotein synthesis (CFGpS) systems using prokaryote cell lysates that are enriched in components for glycoprotein synthesis such as oligosaccharyltransferases (OSTs) and lipid-linked oligosaccharides (LLOs) including OSTs and LLOs associated with synthesis of bacterial O antigens.
专利号:WO-2024012791-A1 优先权日:2022-07-11 标题 :Electrochemical synthesis of pyrazolines and pyrazoles 发明人:BÄR ROBIN MAXIMILIAN; FORD MARK JAMES; KALDAS SHERIF JAMES; WALDVOGEL SIEGFRIED; HOFMANN SILJA; LINDEN MARTIN 权利人:BAYER AG 摘要:The present invention relates to an electrochemical process for the synthesis of pyrazolines and pyrazoles of formula (I). The process can be especially used for the synthesis of the herbicide safener mefenpyr-diethyl.
专利号:WO-2023019298-A1 优先权日:2021-08-20 标 题:Improved method of synthesis of 1-(3',4'-methylene dioxyphenyl)-2-(methylamino) propane (mdma) 发明人:O'MALLEY WILLIAM IAN; WYNNE PAUL MICHAEL 权利人:MIND MEDICINE AUSTRALIA LTD 摘要:The present invention relates to an improved method of synthesis of 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA) that is of sufficient purity that it can be used for pharmaceutical applications. In particular the present invention provides a method of synthesising MDMA comprising the steps of (a) condensation of piperonal and nitroethane in the presence of a catalysing base to form 1-(3',4'-methylenedioxyphenyl)-2-nitroprop-1-ene (MDP-2-nitropropene), (b) oxidative hydrolysis of MDP-2-nitropropene to form 1-(3',4'methylenedioxyphenyl)-propan-2-one (MDP2P), and (c) reductive amination of MDP2P to 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA).
专利号:US-2007088174-A1 优先权日:2005-10-19 标 题 :Synthesis of phenoxyacetic acid derivatives 发明人:WINTER ERIC; REICHEL CARSTEN; GUTHEIL DIETER 权利人:BOEHRINGER INGELHEIM INT 摘要:The present invention relates to an improved process for the preparation of substituted 2-(4-carbonylmethoxy-optionally 2,5-disubstituted-phenyl)-acetaldehydes, in particular 2-(4-alkoxycarbonylmethoxy-optionally 2,5-disubstituted-phenyl)-acetaldehydes and their use in the synthesis of optionally substituted 2-[4-[2-[[-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]-amino]ethyl]-optionally 2,5-disubstituted-phenoxy]acetic acid derivatives or the salts thereof, which may be used as pharmaceutically active substances.
专利号:WO-2025108921-A1 优先权日:2023-11-22 标 题 :Synthesis of radiopharmaceutical agents 发明人:AUZELOUX PHILIPPE; LEVESQUE SOPHIE; GALMIER MARIE-JOSÈPHE; CHEZAL JEAN-MICHEL 权利人:INST NAT SANTE RECH MED; UNIV CLERMONT AUVERGNE; CENTRE LUTTE CONTRE LE CANCER 摘要:Synthesis of radiopharmaceutical agents It is disclosed a method to synthesize a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I), (I) said process comprising contacting a trialkylstannane precursor of formula (II), or a pharmaceutically acceptable salt thereof: Formula (II), (II) with an alkali metal salt of a radionuclide selected from the group consisting of 123I, 124I, 125I, 131I, 211At, in appropriate acidic conditions and in presence of a peroxide ROOH in an 10 appropriate concentration. Said method is particularly suited for synthesizing [131I]N-(2- diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide, providing a notable reduction in the quantity of side products, allowing a much purer finished product, while making use of reagents which are adapted to the constraints which need to be met when developing a product for clinical use and, more in particular, to the constraints to be met in order to 15 adapt the process for being fully automated.