4-溴-5-氟-2-硝基苯甲胺合成路线 (共 10 条)
反应条件
potassium carbonate in methanol 0.5 h;
参考文献
ABBOTT LABORATORIES; KRUEGER, Allan, C.; KATI, Warren, M.; CARROLL, William, A.; PRATT, John, K.; HUTCHINSON, Douglas, K.
Patent: WO2012/83170 A1, 2012 ;
Location in patent: Page/Page column 154-155 ;
反应条件
1: With sulfuric acid; potassium nitrate T=20°C; 2: With hydrogenchloride in tetrahydrofuran; water T=120°C; 0.333333 h; Microwave irradiation; 3: With sodium hydrogencarbonate in tetrahydrofuran; water
参考文献
UCB PHARMA S.A.; BUeRLI, Roland; HAUGHAN, Alan, Findlay; MACK, Stephen, Robert; PERRY, Benjamin, Garfield; RAPHY, Gilles; SAVILLE-STONES, Elizabeth, Anne
Patent: WO2010/52448 A2, 2010 ;
Location in patent: Page/Page column 40-41 ;
WO 2010/052448 A2
反应条件
N-bromosuccinmide; acetic acid 1.5 h; Reflux;
参考文献
F. HOFFMANN-LA ROCHE AG; ALIAGAS-MARTIN, Ignacio; CRAWFORD, James; LEE, Wendy; MATHIEU, Simon; RUDOLPH, Joachim
Patent: WO2013/26914 A1, 2013 ;
Location in patent: Page/Page column 133 ;
WO 2013/026914 A1
反应条件
N-bromosuccinmide in N,N-dimethyl-formamide
参考文献
US5514680 A1, ;
US 5514680 A
反应条件
ammonia in 1,4-dioxane T=70°C; 48 h; regioselective reaction;
参考文献
Journal of Medicinal Chemistry, , vol. 51, # 17 p. 5243 - 5263
反应条件
1.1: 0.5 h / 0 °C 1.2: 0 - 25 °C 2.1: potassium carbonate / methanol / 0.5 h View Scheme
反应条件
1: tin(ll) chloride / ethanol / 14 h / |Reflux 2: |Reflux View Scheme
参考文献
F. HOFFMANN-LA ROCHE AG; ALIAGAS-MARTIN, Ignacio; CRAWFORD, James; LEE, Wendy; MATHIEU, Simon; RUDOLPH, Joachim
Patent: WO2013/26914 A1, 2013 ;
WO 2013/026914 A1
反应条件
tert.-butylnitrite; copper(ll) bromide in acetonitrile
T=60°C;
参考文献
SMITHKLINE BEECHAM CORPORATION
Patent: WO2007/30366 A1, 2007 ;
Location in patent: Page/Page column 121-122 ;
反应条件
iron; ammonium chloride in tetrahydrofuran; ethanol; water
T=95°C; 4 h;
参考文献
ABBOTT LABORATORIES; KRUEGER, Allan, C.; KATI, Warren, M.; CARROLL, William, A.; PRATT, John, K.; HUTCHINSON, Douglas, K.
Patent: WO2012/83170 A1, 2012 ;
Location in patent: Page/Page column 155 ;
反应条件
sodium hydrogencarbonate in ethanol; ethyl acetate
参考文献
The State of Oregon, acting by and through The Oregon State Board of Higher Education, acting for and on behalf of The Oregon Health Sciences University; The University of Oregon; The Regents of the University of California
Patent: US5514680 A1, 1996 ;
US 5514680 A