苯佐卡因置于硫酸体系中,用 甲苯 作为反应溶剂,化学反应 0.5H,反应生成 乙基-4-异叠酸苯酯 参考文献:Organosilicon Synthesis Of Isocyanates: Iii. Synthesis Of Aliphatic,Carbocyclic,Aromatic,And Alkylaromatic Isocyanatocatboxylic Acid Esters 标题:Organosilicon Synthesis Of Isocyanates: Iii. Synthesis Of Aliphatic,Carbocyclic,Aromatic,And Alkylaromatic Isocyanatocatboxylic Acid Esters 摘要:A Series Of Aminoacid Esters Was Prepared By Treating The Aminoacid Suspensions In Ethanol With Thionyl Chloride. Best Conversion Of Aminoacid Esters To Corresponding Isocyanates Was Achieved In The Case Of Aromatic And Carbocyclic Aminoesters By Phosgeneation Of Their N-Silyl Derivatives,And In The Case Of Aliphatic And Alkylaromatic Aminoesters By Phosgeneation Of O-Silyl Or N,O-Bissilylurethanes On Their Basis. In The Last Case Additional Step Of Esterification Of The By-Products Isocyanatoalkylcarboxylic Acid Chlorides Is Reqired After Phosgeneation. Unusual Generation Of Cynnamates And Intramolecular N-> O-Migration Of Trimethylsilyl Group In The Solutions Of Silylated Alkylaromatic Beta-Aminoacid Esters Were Found. DOI:10.1134/s1070363206070115
专利号:WO-9847910-A1 优先权日:1997-04-21 标题:Method for solution phase synthesis of oligonucleotides 发明人:PIEKEN WOLFGANG; MCGEE DANNY; SETTLE ALECIA; ZHAI YANSHENG; HUANG JIANPING; HILL KEN; SMITH RANDALL S 权利人:NEXSTAR PHARMACEUTICALS INC; PIEKEN WOLFGANG; MCGEE DANNY; SETTLE ALECIA; ZHAI YANSHENG; HUANG JIANPING; HILL KEN; SMITH RANDALL S 摘要:This invention discloses an improved method for the sequential solution phase synthesis of oligonucleotides. The method lends itself to automation and is ideally suited for large scale manufacture oligonucleotides with high efficiency.
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:EP-1200395-B1 优先权日:1999-07-28 标 题:Urea derivatives as inhibitors of ccr-3 receptor 发明人:PADIA JANAK; HOCKER MICHAEL D; OHASHI HIROSHI; NISHITOBA TSUYOSHI; SAWA EIJI 权利人:KIRIN BREWERY 摘要:Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.
专利号:US-10570179-B2 优先权日:2016-09-02 标 题:Substituted urea depsipeptide analogs as activators of the CLPP endopeptidase 发明人:LEE RICHARD E; ZHAO YING 权利人:ST JUDE CHILDRENS RES HOSPITAL 摘要:In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-2004106598-A1 优先权日:1998-06-22 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
参考文献:10.2174/1874104500701010011|10.2174/187410450701011105 摘要:Le TC, Berlin KD, Benson SD, Eastman MA, Bell-Eunice G, Nelson AC, Benbrook DM. Heteroarotinoids with anti-cancer activity against ovarian cancer cells. Open Med Chem J. 2007 Oct 24;1():11–23.