反应条件
1.1: boron trichloride / dichloromethane / 0.5 h / -15 °C / Inert atmosphere
1.2: Cooling with ice
2.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / dichloromethane / 0.83 h / 0 °C / Inert atmosphere
3.1: potassium fluoride; sodium bromide / tetrakis(triphenylphosphine) palladium(0) / toluene; water / 18 h / 100 °C / Inert atmosphere
4.1: hydrogenchloride; hydrogen / palladium 10 on activated carbon / ethyl acetate; water / 16 h / 21 °C
5.1: triethylamine / dichloromethane / 2 h / 0 °C / Cooling with ice
6.1: potassium hydroxide; water / ethanol / 1 h / Reflux
View Scheme
参考文献
GLAXO GROUP LIMITED; CHONG, Pek Yoke; MILLER, John F.; PEAT, Andrew James; SHOTWELL, John Brad
Patent: WO2013/28371 A1, 2013 ;