4-氯-6-甲基-2-氧代-1,2-二氢吡啶-3-甲腈置于palladium On Activated Charcoal 氢气体系中,用 甲醇 作为反应溶剂,以88%的收率获得产物3-氰基-6-甲基-2(1H)-吡啶酮 参考文献:Synthesis And Reactions Of 4-Chloro-1,2-Dihydro-6-Methyl-2-Oxo-3-Pyridinecarbonitrile 标题:Synthesis And Reactions Of 4-Chloro-1,2-Dihydro-6-Methyl-2-Oxo-3-Pyridinecarbonitrile 摘要:The Chlorination Of 1,2-Dihydro-4-Hydroxy-6-Methyl-2-Oxo-3-Pyridinecarbonitrile (2) With A Mixture Of Pocl3 And Pcl5 In Chcl3 Gave 4-Chloro-1,2-Dihydro-6-Methyl-2-Oxo-3-Pyridinecarbonitrile (3) In Good Yield. Compound (3) Reacted With Alkyl-And Arylamines To Give The Corresponding 4-Alkylamino-And 4-Arylamino-3-Pyridinecarbonitriles (6 And 7). DOI:10.3987/com-03-9765
专利号:US-6172235-B1 优先权日:1996-08-09 标题 :Asymmetric conjugate addition reaction 发明人:DOLLING ULF H; FREY LISA F; TILLYER RICHARD D; TSCHAEN DAVID M 权利人:MERCK & CO INC 摘要:This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
专利号:US-6514997-B2 优先权日:1999-12-03 标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis 发明人:DRAGOVICH PETER S; PRINS THOMAS J; ZHOU RU; JOHNNSON JR THEODORE O 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the picornaviral 3C protease. Also disclosed are compounds of the formula: n where the formula variables are as defined herein that advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as rhinovirus 3C proteases. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-5521179-A 优先权日:1991-04-18 标题 :Heterocyclic amides 发明人:BERNSTEIN PETER R; SHAW ANDREW; THOMAS ROYSTON M; WARNER PETER; WOLANIN DONALD J 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.
参考标题:Synthesis Of Amido-N-Imidazolium Salts And Their Applications As Ligands In Suzuki-Miyaura Reactions: Coupling Of Hetero- Aromatic Halides And The Synthesis Of Milrinone And Irbesartan 作者:Manian Rajesh Kumar,Kyungho Park,Sunwoo Lee |发布日期:2010.12.17 摘要:Catalytic System Based On Palladium-Amido-N-Heterocyclic Carbenes For Suzuki-Miyaura Coupling Reactions Of Heteroaryl Bromides Is Described. A Variety Of Sterically Bulky, Amido-N-Imidazolium Salts Were Synthesized In High Yields From The Corresponding Anilines. This Catalytic System Effectively Promoted Suzuki-Miyaura Couplings Of Heteroaryl Bromides And Chlorides With A Range Of Boronic Acids To
合成参考文献
摘要:Keller, P. A., Science of Synthesis, (2005) 15, 295. 摘要:Bailey, T. R., Science of Synthesis, (2005) 21, 822.