4-甲氧基苯甲酸甲酯置于4,5-Dichlorophthaloyl Peroxide,碳酸氢钠体系中,用 甲醇,水 作为反应溶剂,以64%的收率获得产物3-羟基-4-甲氧基苯甲酸甲酯 参考文献: Cyclic Peroxide Oxidation Of Aromatic Compound Production And Use Thereof[fr] Oxydation De Peroxyde Cyclique De Production De Composé Aromatique Et Son Utilisation 标题: Cyclic Peroxide Oxidation Of Aromatic Compound Production And Use Thereof[fr] Oxydation De Peroxyde Cyclique De Production De Composé Aromatique Et Son Utilisation 摘要:本发明提供了一种将芳香烃转化为酚的方法,包括提供一种含有一个或多个芳香c-H键和一个或多个活化的c-H键的芳香烃溶剂;向溶剂中添加邻苯二酰过氧化物;将邻苯二酰过氧化物转化为二自由基;将二自由基与一个或多个芳香c-H键接触;优先氧化一个或多个芳香c-H键中的一个,而不是活化的一个或多个c-H键;向一个或多个芳香c-H键中添加一个羟基以形成一个或多个酚;并纯化一个或多个酚.
专利号:EP-1836163-B1 优先权日:2004-12-23 标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin 发明人:BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER 权利人:NOVARTIS AG 摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.
专利号:WO-2011147102-A1 优先权日:2010-05-28 标题 :Synthetic method for 6,7-substituents-4-aniline quinazoline 发明人:SHIH KAE-SHYANG; HSIEH YU-JUNG; LIU CHING-WEI 权利人:SHYANG JEN BIOTECH CO LTD; SHIH KAE-SHYANG; HSIEH YU-JUNG; LIU CHING-WEI 摘要:A method for the synthesis of 6,7-substituents-4-aniline quinazoline is disclosed, in which 3,4-substituted benzoic acid is used as a starting material and 6,7-substituents-4-aniline quinazoline is produced from it by esterification, O-alkylation, nitration, nitro group reduction, cyclization, and two-in-one reaction of chlorination and amine-substitution, or by esterification, O-alkylation or nitration, hydrolysis-demethylation, esterification, O-alkylation, nitro group reduction, cyclization, and two-in-one reaction of chlorination and amine-substitution.
专利号:US-5721099-A 优先权日:1992-10-01 标 题 :Complex combinatorial chemical libraries encoded with tags 发明人:STILL W CLARK; WIGLER MICHAEL H; OHLMEYER MICHAEL H J; DILLARD LAWRENCE W; READER JOHN C 权利人:UNIV COLUMBIA; COLD SPRING HARBOR LAB 摘要:Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
专利号:US-8129411-B2 优先权日:2005-12-30 标题:Organic compounds 发明人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI 权利人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI; NOVARTIS AG 摘要:The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. n The compounds have the formula I′ n nwherein R1, R2, T, R3 and R4 are as defined in the specification.
专利号:US-7807709-B2 优先权日:2005-03-23 标题 :Organic compounds 发明人:EHRHARDT CLAUS; IRIE OSAMU; LORTHIOIS EDWIGE LILIANE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER 权利人:NOVARTIS AG 摘要:The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis.
专利号:US-7691843-B2 优先权日:2002-07-11 标 题 :N-hydroxyamide derivatives possessing antibacterial activity 发明人:RAJU BORE G; O'DOWD HARDWIN; GAO HONGWU; PATEL DINESH V; TRIAS JAOQUIM 权利人:PFIZER 摘要:Novel N-hydroxyamide derivatives are disclosed. These N-hydroxyamide derivatives inhibit UPD-3-O—(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase, an enzyme present in gram negative bacteria and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.
摘要:Wong, Y.-S., Science of Synthesis, (2009) 46, 615. 摘要:Barsegyan, Y. A.; Vil’, V. A.; Tomkinson, N. C. O.; Terent’ev, A. O., Science of Synthesis Knowledge Updates, (2022) 1, 242. 摘要:J. Sunkel and H. Staude, Ber. Bunsenges. Physik. Chem. 72, 567 (1968). 摘要:Angelini, E.; Sarlah, D., Science of Synthesis: Dearomatizations, (2026) . 参考文献:10.1007/s00253-008-1534-y 摘要:Vosmann K, Wiege B, Weitkamp P, Weber N. Preparation of lipophilic alkyl (hydroxy)benzoates by solvent-free lipase-catalyzed esterification and transesterification. Applied Microbiology and Biotechnology. 2008 Jun 10;80(1):29–36. doi: 10.1007/s00253-008-1534-y.