苯佐卡因置于盐酸,Sodium Nitrite,四羟基二硼体系中,用 甲醇,水 作为反应溶剂,化学反应 1.5H,以65%的收率获得产物4-乙氧羰基苯硼酸 参考文献:Methanol-Promoted Borylation Of Arylamines: A Simple And Green Synthetic Method To Arylboronic Acids And Arylboronates 标题:Methanol-Promoted Borylation Of Arylamines: A Simple And Green Synthetic Method To Arylboronic Acids And Arylboronates 摘要:A Sandmeyer Borylation Of Arylamines Via A Sn2Ar Pathway Promoted By Methanol With Sodium Nitrite And Hydrochloric Acid As Diazotization Agent Has Been Developed,Which Provide A Simple And Green Synthetic Method To Arylboronic Acids And Arylboronates. DOI:10.1055/s-0033-1339118
专利号:JP-6038111-B2 优先权日:2014-12-27 标 题:2,6-Dichloro-8-iodo-7-deazapurine for the synthesis of polysubstituted 7-deazapurine derivatives
专利号:US-9938258-B2 优先权日:2012-11-29 标 题:Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof 发明人:BALOGLU ERKAN; SHECHTER SHARON; SHACHAM SHARON; MCCAULEY DILARA; SENAPEDIS WILLIAM; GOLAN GALI; KALID ORI 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula I: n nor a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.
专利号:WO-2009055631-A1 优先权日:2007-10-25 标 题 :Calcilytic compounds 发明人:CASILLAS LINDA N; RAMANJULU JOSHI M; MARQUIS ROBERT W JR 权利人:SMITHKLINE BEECHAM CORP; CASILLAS LINDA N; RAMANJULU JOSHI M; MARQUIS ROBERT W JR 摘要:Novel calcilytic compounds, pharmaceutical compositions, pharmaceutical combinations, methods of synthesis and methods of using them are provided.
专利号:US-8178559-B2 优先权日:2004-12-30 标 题:Organic compounds 发明人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI 权利人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI; NOVARTIS AG 摘要:3,4-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 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
专利号:RU-2197482-C2 优先权日:1997-04-22 标 题 :Substituted phenyl derivatives, method of their synthesis, pharmaceutical composition comprising thereof and method of treatment (variants)
专利号:RU-2150470-C1 优先权日:1994-04-19 标题 :Bicyclic thiophene derivatives, method of their synthesis and composition based on thereof