5-氯吡嗪-2-羧酸甲酯合成路线 （共 29 条）
反应条件
1: 61 percent / nitrobenzene / 3 h / 170 - 180 °C 2: 77 percent / 10percent NaOH / H2O / 3 h / Heating 3: 64 percent / SOCl2 / 2 h / Heating 4: 68 percent / POCl3, DMF / 2 h / Heating View Scheme
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 28, # 10 p. 3057 - 3063
反应条件
1: 64 percent / SOCl2 / 2 h / Heating 2: 68 percent / POCl3, DMF / 2 h / Heating View Scheme
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 28, # 10 p. 3057 - 3063
参考文献
Magnetic Resonance in Chemistry, , vol. 47, # 7 p. 617 - 624
反应条件
bis-(2-hydroxy-ethyl)-amine; trichlorophosphate 2 h; Heating; Yield given. Yields of byproduct given;
参考文献
Journal of Heterocyclic Chemistry, , vol. 31, # 5 p. 1177 - 1180
反应条件
potassium carbonate in tetrahydrofuran; water T=25°C; 42 h;
参考文献
F. HOFFMANN-LA ROCHE AG
Patent: WO2004/52869 A1, 2004 ;
Location in patent: Page 115 - 116 ;
WO 2004/052869 A1
反应条件
1: hexan-1-ol With sodium T=60°C; 0.75 h; 2: 5-chloro-pyrazine-2-carboxylic acid methyl ester T=50°C; 0.583333 h;
参考文献
PHARMACIA and UPJOHN COMPANY
Patent: WO2004/18428 A1, 2004 ;
Location in patent: Page 350-351 ;
反应条件
hydrazine in methanol 48 h; Heating / reflux;
参考文献
Brown, Alan; Ellis, Dave; Pearce, David; Ralph, Michael; Sciammetta, Nunzio
Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 10 p. 2634 - 2636
反应条件
1: With diisobutylaluminium hydride in tetrahydrofuran T=0°C; 2 h; 2: With methanol
参考文献
IRONWOOD PHARMACEUTICALS, INC.; HUDSON, Colleen; BARDEN, Timothy, C.; JIA, James; MERMERIAN, Ara; PENG, Bo; YANG, Jane; YU, Xiang, Y.; SPROTT, Kevin
Patent: WO2012/88469 A1, 2012 ;
Location in patent: Page/Page column 151-152 ;
WO 2012/088469 A1
反应条件
triethylamine in 1,4-dioxane T=45°C; 16 h;
参考文献
US2008/85905 A1, ;
Page/Page column 17 ;
US 20080085905 A1
反应条件
N-ethyl-N,N-diisopropylamine in N,N-dimethyl-formamide T=20°C; 18 h;
参考文献
PFIZER LIMITED; COE, Jotham, Wadsworth; DEHNHARDT, Christoph, Martin; JONES, Peter; KORTUM, Steven Wade; SABNIS, Yogesh, Anil; WAKENHUT, Florian, Michel; WHITLOCK, Gavin, Alistair
Patent: WO2013/14567 A1, 2013 ;
Location in patent: Page/Page column 81 ;
WO 2013/014567 A1
