5-溴-3-甲基-1H-吲唑合成路线 (共 12 条)
反应条件
hydrazine T=117°C; 5 h; Heating / reflux;
参考文献
AMGEN, INC.
Patent: WO2006/44860 A2, 2006 ;
Location in patent: Page/Page column 23-24 ;
WO 2006/044860 A2
反应条件
acetic acid; sodium nitrite in water 4.5 h;
参考文献
AMR TECHNOLOGY, INC.
Patent: WO2008/86404 A1, 2008 ;
Location in patent: Page/Page column 124 ;
WO 2008/086404 A1
反应条件
1: 78 percent / manganese(IV) oxide / dioxane / 4 h / Heating 2: 60 percent / hydrazine monohydrate / 9 h / Heating View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 14, # 20 p. 6832 - 6846
反应条件
1: 99 percent / diethyl ether / 0.5 h / 0 °C 2: 78 percent / manganese(IV) oxide / dioxane / 4 h / Heating 3: 60 percent / hydrazine monohydrate / 9 h / Heating View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 14, # 20 p. 6832 - 6846
反应条件
(1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; triethylamine T=100°C; P=15201 Torr;
参考文献
BIOENERGENIX; MCCALL, John; KELLY, Robert, C.; ROMERO, Donna, L.
Patent: WO2014/66795 A1, 2014 ;
Location in patent: Paragraph 0175 ;
反应条件
1: With potassium acetate in dimethyl sulfoxide 0.25 h; 2: With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride in dimethyl sulfoxide T=86°C; 20 h;
参考文献
US2007/173506 A1, ;
Page/Page column 31; 32 ;
反应条件
1: 5-Bromo-3-methyl-1H-indazole With tert.-butyl lithium in tetrahydrofuran T=-78 - -70°C; 0.75 h; 2: carbon dioxide in tetrahydrofuran T=20°C; 0.833333 h; 3: With hydrogenchloride; sodium hydroxide; water more than 3 stages;
参考文献
AMGEN, INC.
Patent: WO2006/44860 A2, 2006 ;
Location in patent: Page/Page column 23-24 ;
WO 2006/044860 A2
反应条件
1: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium acetate / N,N-dimethyl-formamide / 20 h / 80 °C / 3102.97 Torr 2: water; lithium hydroxide hydrate / methanol / 20 h / 20 °C View Scheme
参考文献
BIOENERGENIX
Patent: US2012/277224 A1, 2012 ;
US 20120277224 A1
反应条件
triethylamine; 4-(N,N-dimethlyamino)pyridine in tetrahydrofuran T=20°C;
参考文献
ALCON MANUFACTURING, LTD.
Patent: US2008/153813 A1, 2008 ;
Location in patent: Page/Page column 24 ;
US 20080153813 A1
反应条件
1: 5-Bromo-3-methyl-1H-indazole With tert.-butyl lithium in tetrahydrofuran; pentane
T=-78 - 70°C; 0.5 h; Inert atmosphere;
2: N,N-dimethyl-formamide in tetrahydrofuran; pentane
T=-78 - 20°C; 2 h; Inert atmosphere;
参考文献
BIGNAN, Gilles; Gaul, Micheal; Xu, Guozhang; Zhao, Bao-Ping
Patent: US2011/150864 A1, 2011 ;
Location in patent: Page/Page column 206 ;