2-{4-[4-(4,4,5,5-四甲基-[1,3,2]二噁硼烷-2-基)-苯基]-1H-咪唑-2-基}-吡咯烷-1-羧酸叔丁酯合成路线 （共 9 条）
反应条件
tetrakis(triphenylphosphine) palladium(0); potassium acetate in 1,4-dioxane T=80°C; Inert atmosphere;
参考文献
MEDIVIR AB; AYESA, Susana; BELDA, Oscar; BJÖRKLUND, Catarina; NILSSON, Magnus; RUSSO, Francesco; SAHLBERG, Christer; WIKTELIUS, Daniel
Patent: WO2013/95275 A1, 2013 ;
Location in patent: Page/Page column 117 ;
反应条件
potassium acetate; tetrakis(triphenylphosphine) palladium(0) in 1,4-dioxane T=80°C; 16.5 h;
参考文献
Bristol-Myers Squibb Company
Patent: US2008/50336 A1, 2008 ;
Location in patent: Page/Page column 65 ;
反应条件
1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 2.5 h / 0 - 20 °C 2.1: ammonium acetate / xylene / 5 h / 130 - 135 °C / Industry scale 3.1: potassium acetate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / 1,4-dioxane / 2 h / Inert atmosphere; Reflux 3.2: pH ~ 8 View Scheme
参考文献
National Health Research Institutes
Patent: US2011/136799 A1, 2011 ;
反应条件
1.1: ammonium acetate / xylene / 5 h / 130 - 135 °C / Industry scale 2.1: potassium acetate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / 1,4-dioxane / 2 h / Inert atmosphere; Reflux 2.2: pH ~ 8 View Scheme
参考文献
PFIZER LIMITED; MILBANK, Jared Bruce John; TRAN, Thien Duc; WAKENHUT, Florian
Patent: WO2011/154871 A1, 2011 ;
反应条件
1: ammonium acetate; acetic acid / xylene / 3 h / 20 - 160 °C 2: potassium acetate / tetrakis(triphenylphosphine) palladium(0) / 1,4-dioxane / 20 - 80 °C / Inert atmosphere View Scheme
参考文献
MEDIVIR AB; AYESA, Susana; BELDA, Oscar; BJÖRKLUND, Catarina; NILSSON, Magnus; RUSSO, Francesco; SAHLBERG, Christer; WIKTELIUS, Daniel
Patent: WO2013/95275 A1, 2013 ;
反应条件
1.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / 0.5 h / 20 °C 1.2: 0.17 h / 20 °C 2.1: ammonium acetate; acetic acid / xylene / 3 h / 20 - 160 °C 3.1: potassium acetate / tetrakis(triphenylphosphine) palladium(0) / 1,4-dioxane / 20 - 80 °C / Inert atmosphere View Scheme
参考文献
National Health Research Institutes
Patent: US2011/136799 A1, 2011 ;
反应条件
1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / dichloromethane / 0 °C 2: ammonium acetate / anhydrous xylene / 4 h / 140 °C / |Sealed tube 3: tetrakis(triphenylphosphine) palladium(0); potassium acetate / 1,4-dioxane / 80 °C / |Inert atmosphere View Scheme
参考文献
MEDIVIR AB; AYESA, Susana; BELDA, Oscar; BJÖRKLUND, Catarina; NILSSON, Magnus; RUSSO, Francesco; SAHLBERG, Christer; WIKTELIUS, Daniel
Patent: WO2013/95275 A1, 2013 ;
反应条件
sodium hydrogencarbonate in ethylene glycol dimethyl ether; water
T=80°C; Suzuki-Miayura coupling; 5.75 h;
参考文献
Bristol-Myers Squibb Company
Patent: US2008/44380 A1, 2008 ;
Location in patent: Page/Page column 73 ;
反应条件
sodium hydrogencarbonate in ethylene glycol dimethyl ether; water
T=80°C; Suzuki-Miayura coupling; 15.5 h;
参考文献
Bristol-Myers Squibb Company
Patent: US2008/44380 A1, 2008 ;
Location in patent: Page/Page column 78 ;
