1-(2-甲氧基-4-硝基苯基)-4-甲基-1H-咪唑合成路线 (共 8 条)
反应条件
1: hydrogen / palladium 10 on activated carbon / ethanol / 3.5 h / 20 °C 2: dichloromethane / 20 °C 3: ammonia / tetrahydrofuran / 0 - 20 °C View Scheme
参考文献
Luebbers, Thomas; Flohr, Alexander; Jolidon, Synese; Jacobsen, Helmut; Ozmen, Laurence; Baumann, Karlheinz; David-Pierson, Pascale
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 21 p. 6554 - 6558
反应条件
hydrogen; palladium 10 on activated carbon in methanol T=20°C; Inert atmosphere of nitrogenCooling with ice-water;
参考文献
BRISTOL-MYERS SQUIBB COMPANY; BOY, Kenneth M.; GUERNON, Jason M.; MACOR, John E.; OLSON, Richard E.; SHI, Jianliang; THOMPSON, III, Lorin A.; WU, Yong-Jin; XU, Li; ZHANG, Yunhui; ZUEV, Dmitry S.
Patent: WO2011/14535 A1, 2011 ;
Location in patent: Page/Page column 44-45 ;
WO 2011/014535 A1
反应条件
1: palladium 10 on activated carbon; hydrogen / ethanol / 4 h / 20 °C / 760.05 Torr 2: ethanol / Reflux View Scheme
参考文献
Luebbers, Thomas; Flohr, Alexander; Jolidon, Synese; Jacobsen, Helmut; Ozmen, Laurence; Baumann, Karlheinz; David-Pierson, Pascale
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 21 p. 6554 - 6558
反应条件
potassium carbonate in dimethyl sulfoxide
T=125°C; 16 h; AutoclaveInert atmosphere;
参考文献
Van Brandt, Sven Franciscus Anna; De Cleyn, Michel Anna Jozef; Gijsen, Henricus Jacobus Maria; Berthelot, Didier Jean-Claude; Surkyn, Michel
Patent: US2012/295891 A1, 2012 ;
Location in patent: Page/Page column 28-29 ;
反应条件
potassium hydroxide in dimethyl sulfoxide
T=80°C; 5 h;
参考文献
F. HOFFMANN-LA ROCHE AG; GOETSCHI, Erwin; JOLIDON, Synese; LUEBBERS, Thomas
Patent: WO2010/40661 A1, 2010 ;
Location in patent: Page/Page column 15 ;
WO 2010/040661 A1
反应条件
sodium hydride in N,N-dimethyl-formamide
T=0 - 70°C; 3 h;
参考文献
Eisai RandD Management Co., Ltd.
Patent: EP2019093 A1, 2009 ;
Location in patent: Page/Page column 50 ;
反应条件
potassium carbonate in N,N-dimethyl-formamide
T=85°C;
参考文献
ASTRAZENECA AB; FORSBLOM, Rickard; PAULSEN, Kim; ROTTICCI, Didier; SANTANGELO, Ellen; WALDMAN, Magnus
Patent: WO2010/53438 A1, 2010 ;
Location in patent: Page/Page column 63 ;
WO 2010/053438 A1
反应条件
1.1: hydrogen; thiophene / palladium 10 on activated carbon / methanol / 50 °C
2.1: sodium nitrite; sulfuric acid; acetic acid / 0.5 h / 10 - 20 °C
2.2: 1 h / 20 °C
View Scheme
参考文献
ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC; DE CLEYN, Michel, Anna, Jozef; VAN BRANDT, Sven, Franciscus, Anna; GIJSEN, Henricus, Jacobus, Maria; BERTHELOT, Didier, Jean-Claude; OEHLRICH, Daniel
Patent: WO2011/86098 A1, 2011 ;
WO 2011/086098 A1