📜哌啶-4-甲酰胺置于lithium Aluminium Tetrahydride,Nabh(Oac)2体系中,用 四氢呋喃,乙腈 作为反应溶剂,化学反应生成 (1-甲基-4-哌啶-)甲胺 参考文献:Discovery Of 5-[5-Fluoro-2-Oxo-1,2-Dihydroindol-(3Z)-Ylidenemethyl]-2,4-Dimethyl-1H-Pyrrole-3-Carboxylic Acid (2-Diethylaminoethyl)Amide,A Novel Tyrosine Kinase Inhibitor Targeting Vascular Endothelial And Platelet-Derived Growth Factor Receptor Tyrosine Kinase 标题:Discovery Of 5-[5-Fluoro-2-Oxo-1,2-Dihydroindol-(3Z)-Ylidenemethyl]-2,4-Dimethyl-1H-Pyrrole-3-Carboxylic Acid (2-Diethylaminoethyl)Amide,A Novel Tyrosine Kinase Inhibitor Targeting Vascular Endothelial And Platelet-Derived Growth Factor Receptor Tyrosine Kinase 摘要:To Improve The Antitumor Properties And Optimize The Pharmaceutical Properties Including Solubility And Protein Binding Of Indolin-2-Ones,A Number Of Different Basic And Weakly Basic Analogues Were Designed And Synthesized. 5-[5-Fluoro-2-Oxo-1,2-Dihydroindol-(3Z)-Ylidenemethyl]-2,4-Dimethyl-1H-Pyrrole-3-Carboxylic Acid (2-Diethylaminoethyl)Amide (12B Or Su11248) Has Been Found To Show The Best Overall Profile In Terms Of Potency For The Vegf-R2 And Pdgf-Rbeta Tyrosine Kinase At Biochemical And Cellular Levels,Solubility,Protein Binding,And Bioavailability. 12B Is Currently In Phase I Clinical Trials For The Treatment Of Cancers. DOI:10.1021/jm0204183
专利号:US-6608196-B2 优先权日:2001-05-03 标题 :Process for solid supported synthesis of pyruvate-derived compounds 发明人:WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L 权利人:GALILEO PHARMACEUTICALS INC 摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
专利号:US-8933227-B2 优先权日:2009-08-14 标题 :Selective synthesis of functionalized pyrimidines 发明人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN 权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.
专利号:US-2002048774-A1 优先权日:1996-11-29 标题 :Liquid phase parallel synthesis of chemical libraries
专利号:US-9982006-B2 优先权日:2014-08-21 标题:2′-chloro aminopyrimidinone and pyrimidine dione nucleosides 发明人:CLARKE MICHAEL O'NEIL HANRAHAN; MACKMAN RICHARD L; SIEGEL DUSTIN 权利人:GILEAD SCIENCES INC 摘要:Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds.
专利号:US-2011190499-A1 优先权日:2009-08-14 标题 :Selective synthesis of functionalized pyrimidines
专利号:US-9828388-B2 优先权日:2014-07-28 标题:Thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-D]pyrimidines useful for treating respiratory syncitial virus infections 发明人:CLARKE MICHAEL O'NEIL HANRAHAN; MACKMAN RICHARD L; SIEGEL DUSTIN 权利人:GILEAD SCIENCES INC 摘要:Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds.