📜3,4-二羟基苯甲醛置于potassium Carbonate,Caesium Carbonate体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 3-环戊氧-4-甲氧基苯甲醛 参考文献:Improving Metabolic Stability Of Phosphodiesterase-4 Inhibitors Containing A Substituted Catechol: Prevention Of Reactive Intermediate Formation And Covalent Binding 标题:Improving Metabolic Stability Of Phosphodiesterase-4 Inhibitors Containing A Substituted Catechol: Prevention Of Reactive Intermediate Formation And Covalent Binding 摘要:A Detailed Study Directed Towards Metabolic Stability Optimization Of The Alkoxy Substituents On The Catechol Moiety Of Cdp-840 Is Reported. Replacement Of The Methoxy And Cyclopentyloxy Substituents By Cyclobutyloxy And/or Difluromethoxy Groups Resulted In The Discovery Of Potent And Selective Pde4 Inhibitors Where The Formation Of Reactive Metabolites That Could Covalently Bind To Microsomal Protein Was Significantly Reduced Or Eliminated. (C) 2002 Elsevier Science Ltd. All Rights Reserved. DOI:10.1016/s0960-894X(02)00349-9
专利号:US-2003073834-A1 优先权日:1997-11-03 标题:Purine compounds having PDE IV inhibitory activity and methods of synthesis 发明人:CAVALLA DAVID J; CHASIN MARK; HOFER PETER 摘要:The present invention comprises compounds having the general formula I: n n n wherein: n Y 1 is N or CH n Z is selected from the group consisting of alkyl groups such as alkylene groups such as CH 2 , CH 2 CH 2 , CH(CH 3 ); alkenyl groups such as CHâ•?CH; alkynyl groups such as C≡C; and NH, N(C 1 -C 3 alkyl), O, S, C(O)CH 2 and OCH 2 ; n R 1 and R 2 are selected from the group consisting of hydrogen and a C 1 -C 8 straight or branched alkyl or a C 3 -C 8 cycloalkyl; n R 3 is a C 1 -C 12 straight or branched alkyl; n R 4 is a C 3 -C 10 cycloalkyl optionally substituted with OH or C 3 -C 10 cycloalkenyl optionally substituted with OH; and n R 8 is a C 1 -C 8 straight or branched alkyl or a C 3 -C 8 cycloalkyl, optionally substituted with OH; n and methods of synthesis.
专利号:WO-0009116-A1 优先权日:1998-08-14 标 题:Grp receptor ligands 发明人:XIANG JIA-NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 权利人:SMITHKLINE BEECHAM CORP; XIANG JIA NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 摘要:Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
专利号:WO-0009115-A1 优先权日:1998-08-14 标 题 :Grp receptor ligands 发明人:XIANG JIA-NING; OSIFO IRENNEGBE KELLY; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 权利人:SMITHKLINE BEECHAM CORP; XIANG JIA NING; OSIFO IRENNEGBE KELLY; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 摘要:Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
专利号:RU-2129554-C1 优先权日:1993-06-21 标题:Derivatives of pyrrolequinolinone, method of their synthesis, intermediate compounds for their synthesis, pharmaceutical composition and method of its preparing
专利号:WO-9929694-A1 优先权日:1997-12-12 标题:Purine compounds having pde iv inhibitory activity and methods of synthesis
专利号:EP-1045850-A1 优先权日:1997-12-12 标题:Purine compounds having pde iv inhibitory activity and methods of synthesis
参考标题:Enantioselective Synthesis Of Pyroglutamic Acid Esters From Glycinate Via Carbonyl Catalysis 作者:Jiguo Ma,Qinghai Zhou,Guanshui Song,Yongchang Song,Guoqing Zhao,Kuiling Ding,Baoguo Zhao |发布日期:2021.5.3 摘要:Direct α‐functionalization Of Nh2‐free Glycinates With Relatively Weak Electrophiles Such As α,β‐unsaturated Esters Still Remains A Big Challenge In Organic Synthesis. With Chiral Pyridoxal 5 D As A Carbonyl Catalyst, Direct Asymmetric Conjugated Addition At The α‐c Of Glycinate 1 A With α,β‐unsaturated Esters 2 Has Been Successfully Realized, To Produce Various Chiral Pyroglutamic Acid Esters 4 In 14-96 %
合成参考文献
摘要:Beingessner, R. L.; Longstreet, A. R.; McTeague, T. A.; Kelly, L. P.; Seo, H.; Tran, T. H.; Wicker, A. C.; Jamison, T. F., Science of Synthesis: Flow Chemistry in Organic Synthesis, (2018) 1, 448. 摘要:Favre-R, Science of Synthesis: Knowledge Updates, (2024) 3, 264. 摘要:Favre-R, Science of Synthesis: Knowledge Updates, (2024) 3, 263.