专利号:WO-2024186075-A1 优先权日:2023-03-03 标题 :Synthesis method of antibody-drug conjugates using proximity effect-based site-selective antibody labeling 发明人:LEE HYUN SOO; KIM SOOIN; KWEON YONGSEOK 权利人:UNIV SOGANG RES & BUSINESS DEVELOPMENT FOUND; RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIV 摘要:The present invention relates to a method for the synthesis of an antibody-drug conjugate using proximity effect-based site-selective antibody labeling. Provided according to the present invention may be a method for the synthesis of an antibody-drug conjugate by site-selectively introducing a drug into an antibody using a pyridinium oxime derivative (labeling mediator protein) introduced into a binding protein containing a non-standard amino acid.
专利号:US-2024294455-A1 优先权日:2021-06-18 标 题:Synthesis of vinylated hydroxy esters with applicability in signal enhanced magnetic resonance imaging 发明人:GLÖGGLER STEFAN; KORCHAK SERGEY; JATAP ANIL P; SAUL PHILIP; MOLL DENIS 权利人:MAX PLANCK GESELLSCHAFT 摘要:The present invention relates to a method for preparing a compound suitable for signal enhanced magnetic resonance imaging comprising the steps of vinylating a mono-, di- or tricarboxylic acid comprising a moiety -Q-Z with Q being O or N and Z being a protecting group by using vinyl acetate, cleaving Z, and if Z has not already been converted into an alcohol upon cleavage, converting Q into an alcohol either by using nitrite or by converting Q into bromine followed by hydrolysis yielding a vinyl hydroxy ester. The compounds used may be partly or fully deuterated. Furthermore, the present invention relates to a vinyl hydroxy ester as well as an intermediate of its synthesis, wherein the vinyl moiety of the vinyl hydroxy ester and of the intermediate is partly or fully deuterated.
专利号:WO-2024174285-A1 优先权日:2023-02-21 标题:Method for preparing halogenated compound from metal halide salt on basis of mobile phase 发明人:SU REN; Ye Jiani 权利人:UNIV SOOCHOW 摘要:Disclosed is a method for preparing a halogenated compound from a metal halide salt on the basis of a mobile phase. The method comprises: converting an aromatic hydrocarbon, alkane or nitrile compound into a halogenated compound by means of a cheap metal halide salt and a photocatalyst under illumination. The method uses a cheap and safe halide salt as a halogen source, does not introduce additional elemental halogen or an additional oxidant, can implement a reaction at normal temperature and normal pressure, is high in terms of selectivity and friendly to environment, and can be used for replacing an existing synthesis reaction system for halogenated compounds. A mobile phase device is used to replace a tank reactor, such that operation is easy and convenient, the price is low, the substrate adaptability is high, the continuous synthesis of halogenated compounds can be achieved, and the method is suitable for industrial large-scale production.
专利号:US-9695109-B2 优先权日:2014-11-04 标题:Telescoping synthesis of 2-methoxymethyl-p-phenylenediamine 发明人:ABEL HEIKE GERTRUD; OSAN ARMIN; SPECKBACHER MARKUS; WEBER INGO REINHOLD; GARRETT GARRY STEVEN 权利人:NOXELL CORP 摘要:A telescoping process for the preparation of 2-methoxymethyl-p-phenylenediamine, a cosmetically acceptable salt thereof, or mixture thereof. The process according to the present invention is a particularly cost effective process in that it avoids sophisticated chemical steps which requires special equipment or expensive catalysts and in that it comprises a recycling step of one of the starting materials, namely 2-methoxymethylaniline.
专利号:US-8193392-B2 优先权日:2005-07-29 标 题:Method for enantioselective synthesis of phosphorus-stereogenic phosphines 发明人:SCRIBAN CORINA; GLUECK DAVID S 权利人:SCRIBAN CORINA; GLUECK DAVID S; DARTMOUTH COLLEGE 摘要:The present invention relates to a process for preparing an enantioenriched phosphorus-stereogenic, tertiary phosphine. Secondary phosphines are contacted with an alkyl halide and base in the presence of a chiral metal catalyst thereby producing the enantioenriched phosphorus-stereogenic, tertiary phosphine for subsequent use in homogeneous catalysis reactions.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
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合成参考文献
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