5-溴-6-氟-1H-吲唑合成路线 （共 7 条）
反应条件
1: With hydrogenchloride in methanol; water T=90°C; 3 h; 2: With sodium hydroxide pH=10;
参考文献
CENTAURUS BIOPHARMA CO., LTD.; XIAO, Dengming; ZHU, Yan; HU, Yuandong; WANG, Huting; LIU, Yuliang; LI, Jijun; SUN, Deguang; WANG, Zhe; WEI, Yongheng; WANG, Zanping; TANG, Guojing; JING, Lutao
Patent: WO2012/103806 A1, 2012 ;
Location in patent: Page/Page column 55 ;
WO 2012/103806 A1
反应条件
1: With tetrakis(triphenylphosphine) palladium(0) in N,N-dimethyl-formamide T=120 - 130°C; 36 h; Inert atmosphere; 2: With water; sodium hydrogencarbonate in ethyl acetate
参考文献
WO2011/72488 A1, ;
Page/Page column 17; 39 ;
WO 2011/072488 A1
反应条件
1.1: chloroform / 20 °C / Cooling with ice 1.2: 16 h / 75 °C 2.1: tetrakis(triphenylphosphine) palladium(0) / N,N-dimethyl-formamide / 36 h / 120 - 130 °C / Inert atmosphere View Scheme
参考文献
WO2011/72488 A1, ;
WO 2011/072488 A1
反应条件
1: acetic acid; bromine / 12 h / 20 °C 2: 18-crown-6 ether; acetic anhydride; potassium acetate / chloroform / 12 h / 65 °C 3: hydrogenchloride / methanol; water / 3 h / 90 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 22, # 1 p. 447 - 458
反应条件
1: toluene / 1 h / |Reflux 2: acetic acid; bromine / 12 h / 20 °C 3: 18-crown-6 ether; acetic anhydride; potassium acetate / chloroform / 12 h / 65 °C 4: hydrogenchloride / methanol; water / 3 h / 90 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 22, # 1 p. 447 - 458
反应条件
1: 18-crown-6 ether; acetic anhydride; potassium acetate / chloroform / 12 h / 65 °C 2: hydrogenchloride / methanol; water / 3 h / 90 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 22, # 1 p. 447 - 458
反应条件
tetrakis(triphenylphosphine) palladium(0) in N,N-dimethyl-formamide
T=115°C; 90 h; Inert atmosphere;
参考文献
GLAXO WELLCOME HOUSE
Patent: US2012/283297 A1, 2012 ;
Location in patent: Page/Page column 23 ;
