1-Boc-4-(3-硝基吡啶-2-基)哌嗪合成路线 （共 9 条）
反应条件
in tetrahydrofuran T=20°C; 2 h;
参考文献
ASTRAZENECA AB
Patent: WO2008/112440 A1, 2008 ;
Location in patent: Page/Page column 46 ;
WO 2008/112440 A1
反应条件
1: 70.9 percent / diisopropylethylamine / CH2Cl2 / 16 h / 20 °C 2: Et3N / CH2Cl2 View Scheme
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 49, # 11 p. 1406 - 1411
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 15, # 21 p. 4867 - 4871
反应条件
1: H2 / 10 percent Pd/C / methanol 2: NaCNBH3 / methanol 3: CF3COOH / CH2Cl2 View Scheme
参考文献
Arjomandi, Omid Khalili; Saemian, Nader; Shirvani, Gholamhossein; Javaheri, Mohsen; Esmailli, Kameh
Journal of Labelled Compounds and Radiopharmaceuticals, 2011 , vol. 54, # 7 p. 363 - 366
反应条件
sodium cyanoborohydride in methanol Ambient temperature;
参考文献
Romero; Morge; Biles; Berrios-Pena; May; Palmer; Johnson; Smith; Busso; Tan; Voorman; Reusser; Althaus; Downey; So; Resnick; Tarpley; Aristoff
Journal of Medicinal Chemistry, 1994 , vol. 37, # 7 p. 999 - 1014
反应条件
1: 1.) acetic anhydride / 1.) 50 deg C - 60 deg C, 2 h, 2.) THF, RT, 18 h 2: 1.) borane dimethyl sulfide complex, 2.) HCl / 1.) THF, reflux, 18 h, 2.) THF, CH3OH, reflux, 1.5 h View Scheme
参考文献
Romero; Morge; Biles; Berrios-Pena; May; Palmer; Johnson; Smith; Busso; Tan; Voorman; Reusser; Althaus; Downey; So; Resnick; Tarpley; Aristoff
Journal of Medicinal Chemistry, 1994 , vol. 37, # 7 p. 999 - 1014
反应条件
hydrogen; palladium on activated charcoal in ethanol P=2534.03 Torr; 6 h;
参考文献
EXELIXIS, INC.; WILLIAMS, Matthew, A.
Patent: WO2012/61337 A1, 2012 ;
Location in patent: Page/Page column 45 ;
WO 2012/061337 A1
反应条件
1: H2 / 10 percent Pd/C / methanol 2: NaCNBH3 / methanol View Scheme
参考文献
Arjomandi, Omid Khalili; Saemian, Nader; Shirvani, Gholamhossein; Javaheri, Mohsen; Esmailli, Kameh
Journal of Labelled Compounds and Radiopharmaceuticals, 2011 , vol. 54, # 7 p. 363 - 366
反应条件
sodium cyanoborohydride; acetic acid 1.) methanol, 0 deg C, 15 min, 2.) methanol, 0 deg C - RT; Yield given. Multistep reaction;
参考文献
Romero; Morge; Biles; Berrios-Pena; May; Palmer; Johnson; Smith; Busso; Tan; Voorman; Reusser; Althaus; Downey; So; Resnick; Tarpley; Aristoff
Journal of Medicinal Chemistry, 1994 , vol. 37, # 7 p. 999 - 1014
