2-氯-4-(2-氟吡啶-4-基)嘧啶合成路线 (共 3 条)
反应条件
dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct; sodium carbonate in 1,4-dioxane; water T=80°C; Suzuki Coupling; 3 h; Inert atmosphere;
参考文献
ARRAY BIOPHARMA INC.; GENENTECH, INC.; BLAKE, James F.; CHICARELLI, Mark Joseph; GARREY, Rustam Ferdinand; GAUDINO, John; GRINA, Jonas; MORENO, David A.; MOHR, Peter J.; REN, Li; SCHWARZ, Jacob; CHEN, Huifen; ROBARGE, Kirk; ZHOU, Aihe
Patent: WO2013/130976 A1, 2013 ;
Location in patent: Paragraph 00262 ;
反应条件
1: 2-fluoro-4-iodo-pyridine With n-butyllithium; zinc(II) chloride in tetrahydrofuran T=-70°C; 2: 4,6-dichloro-pyrimidine With tetrakis(triphenylphosphine) palladium(0) in tetrahydrofuran Negishi cross-coupling; Heating;
参考文献
Stanetty, Peter; Hattinger, Gregor; Schnuerch, Michael; Mihovilovic, Marko D.
Journal of Organic Chemistry, 2005 , vol. 70, # 13 p. 5215 - 5220
反应条件
1: 2-fluoro-4-iodo-pyridine With n-butyllithium in tetrahydrofuran; hexane T=-70°C; 0.333333 h; 2: With zinc(II) iodide in tetrahydrofuran; hexane T=-60 - 20°C; 1 h; 3: 2,4-Dichloro-pyrimidine With tetrakis(triphenylphosphine) palladium(0) T=110°C; Negishi reaction; 0.0833333 h; microwave irradiation;
参考文献
Stanetty, Peter; Schnuerch, Michael; Mihovilovic, Marko D.
Synlett, 2003 , # 12 p. 1862 - 1864