📜Tert-Butyl (1-Phenylcyclopropyl)Carbamate置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 1.5H,以62%的收率获得产物1-苯基-1-环丙羧酸 参考文献: Kinase Inhibitors And Method Of Treating Cancer With Same[fr] Inhibiteurs De Kinases Et Procédé De Traitement Du Cancer Utilisant Ceux-Ci 标题: Kinase Inhibitors And Method Of Treating Cancer With Same[fr] Inhibiteurs De Kinases Et Procédé De Traitement Du Cancer Utilisant Ceux-Ci 摘要:本教学提供了一种由结构式(I)表示的化合物,或其药用可接受的盐.还描述了一种药物组合物及其使用方法.
专利号:US-10899695-B2 优先权日:2017-02-06 标 题 :Process for the synthesis of 1-aryl-1-trifluoromethylcyclopropanes 发明人:MCLAREN LEE; TO DANIEL; TOVELL DAVID; ABELE STEFAN 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to a process for the manufacturing of 1-aryl-1-trifluoromethylcyclopropanes, which serve as intermediates for the manufacturing of calcium T channel blockers of the general formula (A) n nwhich are described in WO 2015/186056.
专利号:US-6664282-B2 优先权日:1999-09-17 标 题:Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds 发明人:ELABDELLAOUI HASSAN M; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
专利号:US-7309799-B2 优先权日:2004-06-01 标 题:Methods for the synthesis of milnacipran and congeners thereof 发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V 权利人:COLLEGIUM PHARMACEUTICAL INC 摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
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-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-5856107-A 优先权日:1997-02-04 标 题 :Combinatorial libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene derivatives, methods of making the libraries and compounds therein 发明人:OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene compounds. The present invention further provides methods of preparing the libraries and the individual compounds made by the combinatorial synthesis.
[参考文献]: Radoslaw Laufer, Et Al. Discovery Of Inhibitors Of The Mitotic Kinase Ttk Based On N-(3-(3-Sulfamoylphenyl)-1H-Indazol-5-Yl)-Acetamides And Carboxamides. Bioorg Med Chem. 2014 Sep 1;22(17):4968-97.