间溴苯酚置于[1,3-双(二苯基膦基)丙烷]二氯化钯(II) 吡啶体系中,用 四氢呋喃 用作溶剂,化学反应 11.0H,反应生成3-溴联苯 参考文献:Aryl Bromide/triflate Selectivities Reveal Mechanistic Divergence In Palladium-Catalysed Couplings; The Suzuki-miyaura Anomaly 标题:Aryl Bromide/triflate Selectivities Reveal Mechanistic Divergence In Palladium-Catalysed Couplings; The Suzuki-miyaura Anomaly 摘要:在催化交叉反应中,和三之间的竞争的结果取决于核性伴侣;苏苏基与r.b的交叉通常跟随其他r.m物种的不同模式. Doi:10.1039/b701517H
专利信息
专利号:US-5254776-A 优先权日:1992-07-17 标 题:Synthesis of bromobiphenyls 发明人:LANG JOHN F; GURUSAMY NARAYANASAMY 权利人:MALLINCKRODT SPEC CHEM 摘要:Bromobiphenyls (such as 2-fluoro-4-bromobiphenyl) are synthesized by reacting together a phenylboronic acid (such as phenylboronic acid) and a bromoiodobenzene (such as 2-fluoro-4-bromoiodobenzene). The reaction generally takes place with the aid of a catalyst (such as palladium in a zero valance state) and an inert solvent (such as fluorobenzene). Control of temperature is very important to obtain both an acceptable reaction rate and an acceptable level of terphenyl byproduct.
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.
专利号:US-6849650-B2 优先权日:1998-02-27 标 题:Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THORSETT EUGENE D; PORTER WARREN J; NISSEN JEFFREY S; LATIMER LEE H; AUDIA JAMES E; DROSTE JAMES 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 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 comprising 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.
专利号:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-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 权利人:LILLY CO ELI 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.
专利号:US-7390801-B2 优先权日:1996-12-23 标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THORSETT EUGENE D; PLEISS MICHAEL A; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES A; REEL JON K; DRESSMAN BRUCE A; DROSTE JAMES J; HENRY STEVEN S; STUCKY RUSSELL D; PORTER WARREN J 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 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 comprising 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.
专利号:US-11028082-B2 优先权日:2017-05-30 标题 :Process for the preparation of a novel umeclidinium synthesis intermediate 发明人:BERTOLINI GIORGIO; COLLI CORRADO; NISIC FILIPPO; SADA MARA; BERTUOLO STEFANIA; RONZONI SILVANO; MAIORANA STEFANO; DI FABIO ROMANO 权利人:OLON SPA 摘要:The present invention relates to a process for the preparation of a novel and versatile synthesis intermediate and its use in the preparation of umeclidinium. The invention also relates to some reference standards allowing to detect impurity traces recurring in the preparation of umeclidinium and a process for their preparation.
参考标题:Novel Diarylurea Based Allosteric Modulators Of The Cannabinoid Cb1 Receptor: Evaluation Of Importance Of 6-Pyrrolidinylpyridinyl Substitution 作者:Thuy Nguyen,Nadezhda German,Ann M. Decker,Tiffany L. Langston,Thomas F. Gamage,Charlotte E. Farquhar,Jun-Xu Li,Jenny L. Wiley,Brian F. Thomas,Yanan Zhang |发布日期:2017.9.14 摘要:Allosteric Modulators Of The Cannabinoid Cb1 Receptor Have Recently Been Reported As An Alternative Approach To Modulate The Cb1 Receptor For Therapeutic Benefits. In This Study, We Report The Design And Synthesis Of A Series Of Diarylureas Derived From Psncbam-1 (2). Similar To 2, These Diarylureas Dose-Dependently Inhibited Cp55,940-Induced Intracellular Calcium Mobilization And [35S]Gtp-γ-S Binding
合成参考文献
摘要:Eichman, C. C.; Stambuli, J. P., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 367. 摘要:Shi, L., Science of Synthesis: Knowledge Updates, (2024) 1, 22. 摘要:Cheng, Q.; Shen, X., Science of Synthesis: Knowledge Updates, (2025) 2.