2-甲氧基-5-硝基-6-甲基吡啶合成路线 （共 15 条）
反应条件
1: 2.) H2 / 2.) Pd/C / 1.) reflux, 3 h, 2.) toluene 2: 1.) phosphorus oxychloride, 2.) conc. HCl / 1.) 0 deg C, 1 h, 2.) MeOH, THF, RT, 45 min 3: 94 percent / HBr / acetic acid / 2 h / 100 °C View Scheme
参考文献
Buchheit; Gamse; Giger; Hoyer; Klein; Kloeppner; Pfannkuche; Mattes
Journal of medicinal chemistry, 1995 , vol. 38, # 13 p. 2331 - 2338
反应条件
1: 2.) H2 / 2.) Pd/C / 1.) reflux, 3 h, 2.) toluene 2: 1.) phosphorus oxychloride, 2.) conc. HCl / 1.) 0 deg C, 1 h, 2.) MeOH, THF, RT, 45 min View Scheme
参考文献
Buchheit; Gamse; Giger; Hoyer; Klein; Kloeppner; Pfannkuche; Mattes
Journal of medicinal chemistry, 1995 , vol. 38, # 13 p. 2331 - 2338
反应条件
1: Et3N / dimethylformamide / 2 h / 120 °C 2: 19.6 g / H2 / 10 percent Pd/C / ethanol / 4 h / 20 °C / 2068.59 Torr View Scheme
参考文献
Filla, Sandra A.; Mathes, Brian M.; Johnson, Kirk W.; Phebus, Lee A.; Cohen, Marlene L.; Nelson, David L.; Zgombick, John M.; Erickson, Jon A.; Schenck, Kathryn W.; Wainscott, David B.; Branchek, Theresa A.; Schaus, John M.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 14 p. 3060 - 3071
反应条件
hydrogen; palladium on activated charcoal 1.) reflux, 3 h, 2.) toluene; Yield given. Multistep reaction;
参考文献
Buchheit; Gamse; Giger; Hoyer; Klein; Kloeppner; Pfannkuche; Mattes
Journal of medicinal chemistry, 1995 , vol. 38, # 13 p. 2331 - 2338
反应条件
1.1: ethanol; potassium / 0.08 h
1.2: 36 h / 20 °C
2.1: AlCl3, aluminium chloride; sodium tetrahydroborate / ethyl acetate; methanol / 4 h / 0 °C
3.1: hydrogen / palladium 10 on activated carbon / methanol / 16 h / 20 °C / 2068.65 Torr
4.1: phosphorus oxytribromide / N,N-dimethyl-formamide / 0.33 h / Reflux
4.2: pH 7 - 8
View Scheme
参考文献
MERCK and CO., INC.
Patent: WO2009/155156 A1, 2009 ;
WO 2009/155156 A1
