6-溴-1H-吡唑并[4,3-b]吡啶合成路线 (共 12 条)
反应条件
1: With potassium acetate; acetic anhydride; acetic acid in chloroform T=20°C; 0.25 h; 2: With isopentyl nitrite in chloroform T=40 - 60°C; 3: With sodium hydroxide in methanol; water T=0 - 20°C;
参考文献
Pfizer Inc
Patent: US2012/108619 A1, 2012 ;
Location in patent: Page/Page column 30 ;
反应条件
1: With potassium acetate; acetic anhydride in chloroform T=20°C; 5 h; Reflux; 2: With 18-crown-6 ether; isopentyl nitrite in chloroform T=20°C; 26 h; Reflux; 3: With potassium carbonate in methanol; water T=0°C; 2 h;
参考文献
US2010/125089 A1, ;
Page/Page column 89 ;
反应条件
hydrazine hydrate in ethylene glycol T=140°C; 23 h;
参考文献
Sato Pharmaceutical Co., Ltd.; NAGAI Keita; NAGASAWA Koh; TAKAHASHI Hirobumi; BABA Motoaki; FUJIOKA Shinichi; KONDOH Eri; TANAKA Kenichi; ITOH Yoshiki
Patent: EP2669270 A1, 2013 ;
Location in patent: Paragraph 0952-0953 ;
反应条件
methanol; potassium carbonate 1 h; Reflux;
参考文献
WO2012/87782 A1, ;
Page/Page column 75 ;
WO 2012/087782 A1
反应条件
1.1: hydrogenchloride; iron / ethanol; water / 40 °C / Reflux 2.1: triethylamine / dichloromethane / 0 - 20 °C 3.1: acetic anhydride; potassium acetate; acetic acid / chloroform / 0.25 h / 20 °C 3.2: 40 - 60 °C 3.3: 0 - 20 °C View Scheme
反应条件
1.1: hydrogenchloride; water / 18 h / Reflux 1.2: 0 °C 2.1: hydrogenchloride; iron / ethanol; water / 40 °C / Reflux 3.1: triethylamine / dichloromethane / 0 - 20 °C 4.1: acetic anhydride; potassium acetate; acetic acid / chloroform / 0.25 h / 20 °C 4.2: 40 - 60 °C 4.3: 0 - 20 °C View Scheme
反应条件
1.1: sodium hydride / N,N-dimethyl-formamide / 0 - 20 °C 1.2: 2 h / 100 °C 2.1: hydrogenchloride; water / 18 h / Reflux 2.2: 0 °C 3.1: hydrogenchloride; iron / ethanol; water / 40 °C / Reflux 4.1: triethylamine / dichloromethane / 0 - 20 °C 5.1: acetic anhydride; potassium acetate; acetic acid / chloroform / 0.25 h / 20 °C 5.2: 40 - 60 °C 5.3: 0 - 20 °C View Scheme
反应条件
1.1: diisobutylaluminium hydride / dichloromethane; toluene / -78 - 0 °C 1.2: -78 °C 2.1: hydrazine hydrate / ethylene glycol / 23 h / 140 °C View Scheme
反应条件
triethylamine; 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl; palladium dichloride in acetonitrile T=100°C; P=15001.5 Torr; 18 h;
参考文献
Pfizer Inc
Patent: US2012/108619 A1, 2012 ;
Location in patent: Page/Page column 30 ;
反应条件
1.1: triethylamine / 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl; palladium dichloride / acetonitrile / 18 h / 100 °C / 15001.5 Torr 2.1: sodium hydroxide; water / methanol / 0 - 20 °C 2.2: pH 5 - 6 View Scheme
参考文献
Pfizer Inc
Patent: US2012/108619 A1, 2012 ;