2,6-二氯-5-氟烟酸置于palladium Diacetate,N,N-二甲基甲酰胺,三苯基膦 甲酸,草酰氯,一水合肼,三乙胺,三氟乙酸酐体系中,用 二氯甲烷,N,N-二甲基甲酰胺,正丁醇 用作溶剂,化学反应 5.5H,反应生成3-氨基-5-氟-1H-吡唑[3,4-B]吡啶 参考文献:Aminopyrimidines Useful As Inhibitors Of Protein Kinases 标题:Aminopyrimidines Useful As Inhibitors Of Protein Kinases 摘要:本发明涉及用作蛋白激酶抑制剂的化合物.该发明还提供包含这些化合物的药用合适组合物,以及在治疗各种疾病,症状和障碍中使用这些化合物和组合物的方法.该发明还提供制备本发明化合物的方法.
专利信息
专利号:US-8598361-B2 优先权日:2007-07-31 标题 :Process for preparing 5-fluoro-1H-pyrazolo [3,4-B] pyridin-3-amine and derivatives therof 发明人:JIMENEZ JUAN-MIGUEL; MILLER ANDREW; COLLIER PHILIP; GREEN JEREMY; DROS ALBERT; GAO HUAI; HAMON SYLVAIN 权利人:JIMENEZ JUAN-MIGUEL; MILLER ANDREW; COLLIER PHILIP; GREEN JEREMY; DROS ALBERT; GAO HUAI; HAMON SYLVAIN; VERTEX PHARMA 摘要:The present invention relates to a process for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine in high yield and purity. The present invention also relates to processes for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives. These processes are useful for preparing biologically active compounds, particularly certain GSK-3 inhibitors, or derivatives thereof.
专利号:US-2013211090-A1 优先权日:2010-09-03 标题:Method for the production of 5-fluoro-1h-pyrazolo[3,4-b]pyridine-3-carbonitrile 发明人:FOLLMANN MARKUS; ACKERSTAFF JENS 权利人:FOLLMANN MARKUS; ACKERSTAFF JENS; BAYER IP GMBH 摘要:The present invention relates to a process for preparing 5-fluoro-1H-pyrazolo[3,4-b]pyridine-3-carbonitrile of the formula (I) n n n n n n n n n n which serves as a synthesis intermediate for production of medicaments, especially for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
参考标题: Process For Preparing 5-Fluoro-1H-Pyrazolo [3, 4-B] Pyridin-3-Amine And Derivatives Thereof Procédé De Préparation De La 5-Fluoro-1H-Pyrazolo[3,4-B]Pyridin-3-Amine Et Des Dérivés De Celle-Ci 摘要:The Present Invention Relates To A Process For The Synthesis Of 5-Fluoro-1H-Pyrazolo [3, 4-B]Pyridin-3-Amine In High Yield And Purity. The Present Invention Also Relates To Processes For The Synthesis Of 5-Fluoro-1H-Pyrazolo [3, 4- B] ρyridin-3-Amine Derivatives. These Processes Are Useful For Preparing Biologically Active Compounds, Particularly Certain Gsk-3 Inhibitors, Or Derivatives Thereof. Reagents And Conditi Ons : I. Pd ( Oac )2, Pph3, Et3N, H2Co2; I I. 1 ) (Cocl )2, Ch2Cl2, Cat. Dmf; 2 ) Nh3 (G ), Dioxane, I I I. Tfaa, Et3N, Ch2Cl2, O°C; Iv. H2Nnh2. H2O, N-Butanol, Reflux.