3-(叔丁氧基羰基)-苯硼酸合成路线 (共 3 条)
反应条件
1.1: potassium carbonate / toluene; water / 1 h / 65 °C / |Inert atmosphere 1.2: 2 h / 80 °C 2.1: urea hydrogen peroxide addition compound; phthalic anhydride / ethyl acetate; water / 4 h / 45 °C 3.1: pyridine; trifluoromethanesulfonic anhydride / acetonitrile / 1 h / 70 - 75 °C 3.2: 2 h View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; VERWIJS, Marinus, Jacobus; KARKARE, Radhika; MOORE, Michael, Douglas
Patent: WO2014/71122 A1, 2014 ;
反应条件
1.1: potassium carbonate / toluene; water / 1 h / 65 °C / |Inert atmosphere 1.2: 2 h / 80 °C / |Inert atmosphere 2.1: urea hydrogen peroxide addition compound; phthalic anhydride / water; ethyl acetate / 45 °C 3.1: trifluoromethanesulfonic anhydride; pyridine / acetonitrile / 1.33 h / 70 - 75 °C 3.2: 2 h / 20 °C 4.1: triethylamine; 4-(N,N-dimethlyamino)pyridine / toluene / 2 h 5.1: hydrogenchloride; water / acetonitrile / 40 - 45 °C View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; VERWIJS, Marinus, Jacobus; KARKARE, Radhika; MOORE, Michael, Douglas
Patent: WO2014/71122 A1, 2014 ;
反应条件
1: 2-bromo-3-methyl-pyridine With potassium carbonate in water; toluene
T=65°C; 1 h;
2: 3-(tert-butoxycarbonyl)phenylboronic acid With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride in water; toluene
T=80°C; 2 h;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2009/76142 A2, 2009 ;
Location in patent: Page/Page column 53-54 ;