3-溴-5-甲基-4-氮杂吲哚合成路线 (共 5 条)
反应条件
1: With copper(ll) bromide in acetonitrile T=20°C; 1 h; 2: With ammonium hydroxide in methanol; acetonitrile T=20°C; 0.5 h;
参考文献
Almirall, S.A.; Vidal Juan, Bernat; Alonso Diez, Juan Antonio; Buil Albero, María Antonia; Eastwood, Paul Robert; Esteve Trias, Cristina; Lozoya Toribio, María Estrella; Roberts, Richard Spurring; Vidal Gispert, Laura
Patent: EP2548876 A1, 2013 ;
Location in patent: Paragraph 0291-0294 ;
EP 2548876 A1
反应条件
1.1: sodium hydroxide; tetrakis(triphenylphosphine) palladium(0) / tetrahydrofuran / 24 h / 65 °C / |Inert atmosphere 2.1: hydrogenchloride / methanol / 21 h / 75 °C 3.1: potassium carbonate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / ethylene glycol diethyl ether / 1 h / 120 °C / |Inert atmosphere; |Microwave irradiation 4.1: copper(ll) bromide / acetonitrile / 1 h / 20 °C 4.2: 0.5 h / 20 °C View Scheme
参考文献
Almirall, S.A.; Vidal Juan, Bernat; Alonso Diez, Juan Antonio; Buil Albero, María Antonia; Eastwood, Paul Robert; Esteve Trias, Cristina; Lozoya Toribio, María Estrella; Roberts, Richard Spurring; Vidal Gispert, Laura
Patent: EP2548876 A1, 2013 ;
EP 2548876 A1
反应条件
1.1: hydrogenchloride / methanol / 21 h / 75 °C 2.1: potassium carbonate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / ethylene glycol diethyl ether / 1 h / 120 °C / |Inert atmosphere; |Microwave irradiation 3.1: copper(ll) bromide / acetonitrile / 1 h / 20 °C 3.2: 0.5 h / 20 °C View Scheme
参考文献
Almirall, S.A.; Vidal Juan, Bernat; Alonso Diez, Juan Antonio; Buil Albero, María Antonia; Eastwood, Paul Robert; Esteve Trias, Cristina; Lozoya Toribio, María Estrella; Roberts, Richard Spurring; Vidal Gispert, Laura
Patent: EP2548876 A1, 2013 ;
EP 2548876 A1
反应条件
1.1: potassium carbonate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / ethylene glycol diethyl ether / 1 h / 120 °C / |Inert atmosphere; |Microwave irradiation 2.1: copper(ll) bromide / acetonitrile / 1 h / 20 °C 2.2: 0.5 h / 20 °C View Scheme
参考文献
Almirall, S.A.; Vidal Juan, Bernat; Alonso Diez, Juan Antonio; Buil Albero, María Antonia; Eastwood, Paul Robert; Esteve Trias, Cristina; Lozoya Toribio, María Estrella; Roberts, Richard Spurring; Vidal Gispert, Laura
Patent: EP2548876 A1, 2013 ;
EP 2548876 A1
反应条件
1.1: N-iodo-succinimide / N,N-dimethyl-formamide / 16 h / 20 °C 2.1: sodium hydroxide; tetrakis(triphenylphosphine) palladium(0) / tetrahydrofuran / 24 h / 65 °C / |Inert atmosphere 3.1: hydrogenchloride / methanol / 21 h / 75 °C 4.1: potassium carbonate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / ethylene glycol diethyl ether / 1 h / 120 °C / |Inert atmosphere; |Microwave irradiation 5.1: copper(ll) bromide / acetonitrile / 1 h / 20 °C 5.2: 0.5 h / 20 °C View Scheme
参考文献
Almirall, S.A.; Vidal Juan, Bernat; Alonso Diez, Juan Antonio; Buil Albero, María Antonia; Eastwood, Paul Robert; Esteve Trias, Cristina; Lozoya Toribio, María Estrella; Roberts, Richard Spurring; Vidal Gispert, Laura
Patent: EP2548876 A1, 2013 ;
EP 2548876 A1