4-(1H-吡唑-4-基)-7-((2-(三甲基甲硅烷基)乙氧基)-甲基)-7h-吡咯并[2,3-d]嘧啶合成路线 (共 10 条)
反应条件
potassium carbonate; tetrakis(triphenylphosphine) palladium(0) in 1,4-dioxane; water T=90°C; 2 h; Inert atmosphere;
参考文献
Zhou, Jiacheng; Liu, Pingli; Lin, Qiyan; Metcalf, Brian W.; Meloni, David; Pan, Yongchun; Xia, Michael; Li, Mei; Yue, Tai-Yuen; Rodgers, James D.; Wang, Haisheng
Patent: US2010/190981 A1, 2010 ;
Location in patent: Page/Page column 75-76 ;
US 20100190981 A1
反应条件
potassium tert-butylate in tetrahydrofuran; acetonitrile T=0 - 20°C; Inert atmosphere;
参考文献
Zhou, Jiacheng; Liu, Pingli; Lin, Qiyan; Metcalf, Brian W.; Meloni, David; Pan, Yongchun; Xia, Michael; Li, Mei; Yue, Tai-Yuen; Rodgers, James D.; Wang, Haisheng
Patent: US2010/190981 A1, 2010 ;
Location in patent: Page/Page column 84-85 ;
US 20100190981 A1
反应条件
water; potassium carbonate; tetrakis(triphenylphosphine) palladium(0) in butan-1-ol T=100°C; Inert atmosphere;
参考文献
US2011/224190 A1, ;
Page/Page column 37-38 ;
US 20110224190 A1
反应条件
hydrogenchloride; water in tetrahydrofuran T=20°C; Inert atmosphereLarge scale reaction;
参考文献
Lin, Qiyan; Meloni, David; Pan, Yongchun; Xia, Michael; Rodgers, James; Shepard, Stacey; Li, Mei; Galya, Laurine; Metcalf, Brian; Yue, Tai-N; Liu, Pingli; Zhou, Jiacheng
Organic Letters, 2009 , vol. 11, # 9 p. 1999 - 2002
反应条件
1.1: sodium hydride / isobutyramide; mineral oil / 1 h / -5 - 0 °C 1.2: 1 h / 0 °C 2.1: potassium carbonate; water / tetrakis(triphenylphosphine) palladium(0) / butan-1-ol / 100 °C / Inert atmosphere View Scheme
参考文献
US2011/224190 A1, ;
US 20110224190 A1
反应条件
1.1: sodium hydride / isobutyramide; mineral oil / 1 h / -5 - 0 °C 1.2: 1 h / 0 °C 2.1: potassium carbonate; water / tetrakis(triphenylphosphine) palladium(0) / butan-1-ol / 100 °C / Inert atmosphere View Scheme
参考文献
US2011/224190 A1, ;
US 20110224190 A1
反应条件
1: potassium carbonate; tetrakis(triphenylphosphine) palladium(0) / water; butan-1-ol / 90 °C / |Inert atmosphere; |Large scale 2: hydrogenchloride / water; tetrahydrofuran / 16 - 30 °C / |Large scale View Scheme
反应条件
1: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 20 °C 2: ethanol; hexane / |Resolution of racemate 3: trifluoroacetic acid / dichloromethane / 6 h 4: isopropyl alcohol / 20 °C / |Heating View Scheme
反应条件
1: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 20 °C 2: ethanol; hexane / |Resolution of racemate 3: trifluoroacetic acid / dichloromethane / 6 h View Scheme
参考文献
NOVARTIS PHARMA AG; INCYTE CORPORATION; VANNUCCHI, Alessandro M.; BOGANI, Costanza; BARTALUCCI, Niccolo
Patent: WO2013/23119 A1, 2013 ;
反应条件
1: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 20 °C 2: ethanol; hexane / |Resolution of racemate 3: trifluoroacetic acid / dichloromethane / 6 h 4: phosphoric acid / isopropyl alcohol / 20 °C / |Heating View Scheme