1-[(4-甲基苯基)磺酰基]-4-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)-1H-吡咯并[2,3-b]吡啶合成路线 （共 4 条）
反应条件
potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride in ethylene glycol dimethyl ether T=160°C; 0.333333 h; microwave irradiatuon; Product distribution / selectivity;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2006/127587 A1, 2006 ;
Location in patent: Page/Page column 86 ;
WO 2006/127587 A1
反应条件
1.1: [14C]-Tetramethylammonium bromide; trifluoromethanesulfonic anhydride / N,N-dimethyl-formamide / 24.5 h / 0 - 20 °C / Inert atmosphere 1.2: pH 7 2.1: sodium hydroxide / tetra(n-butyl)ammonium hydrogensulfate / dichloromethane / 1 h / 20 °C 3.1: potassium acetate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / N,N-dimethyl-formamide / 24 h / 90 °C / Inert atmosphere View Scheme
反应条件
1.1: n-heptane; ethylene glycol dimethyl ether / 19 h / 20 °C / Inert atmosphere 2.1: potassium carbonate / water / 2 h / 20 °C / pH 10 3.1: [14C]-Tetramethylammonium bromide; trifluoromethanesulfonic anhydride / N,N-dimethyl-formamide / 24.5 h / 0 - 20 °C / Inert atmosphere 3.2: pH 7 4.1: sodium hydroxide / tetra(n-butyl)ammonium hydrogensulfate / dichloromethane / 1 h / 20 °C 5.1: potassium acetate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / N,N-dimethyl-formamide / 24 h / 90 °C / Inert atmosphere View Scheme
反应条件
1: sodium hydroxide / tetra(n-butyl)ammonium hydrogensulfate / dichloromethane / 1 h / 20 °C 2: potassium acetate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / N,N-dimethyl-formamide / 24 h / 90 °C / Inert atmosphere View Scheme
