3-氨基-2-甲氧基吡啶-5-硼酸频哪醇酯合成路线 （共 9 条）
反应条件
potassium acetate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct in 1,4-dioxane T=20 - 100°C;
参考文献
GLAXOSMITHKLINE LLC; BOTYANSZKI, Janos; DICKERSON, Scott Howard; LEIVERS, Martin Robert; LI, Xiaofei; MCFADYEN, Robert Blount; REDMAN, Aniko Maria; SHOTWELL, John Bradford; XUE, Jianjun
Patent: WO2012/174312 A2, 2012 ;
Location in patent: Page/Page column 287 ;
WO 2012/174312 A2
反应条件
hydrogen; Raney-Ni in methanol 2 h;
参考文献
Su, Weiguo; Zhang, Weihan; Yang, Haibin
Patent: US2013/190307 A1, 2013 ;
Location in patent: Paragraph 0151; 0152 ;
反应条件
hydrogen; palladium hydroxide on carbon in methanol T=20°C; 5 h;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2006/65946 A1, 2006 ;
Location in patent: Page/Page column 72 ;
WO 2006/065946 A1
反应条件
1: hydrogenchloride; iron / ethanol; water / 23 h / 10 - 25 °C / Industry scale; Inert atmosphere 2: potassium acetate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / 1,4-dioxane / 2 h / 80 °C / Inert atmosphere View Scheme
参考文献
WO2012/32067 A1, ;
WO 2012/032067 A1
反应条件
1: potassium acetate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / 1,4-dioxane / 2 h / Reflux 2: hydrogen / Raney-Ni / methanol / 2 h / 20 °C View Scheme
参考文献
WO2012/34526 A1, ;
WO 2012/034526 A1
反应条件
1: methanol / 2.75 h / 0 - 10 °C / Industry scale; Inert atmosphere 2: hydrogenchloride; iron / ethanol; water / 23 h / 10 - 25 °C / Industry scale; Inert atmosphere 3: potassium acetate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / 1,4-dioxane / 2 h / 80 °C / Inert atmosphere View Scheme
参考文献
WO2012/32067 A1, ;
WO 2012/032067 A1
反应条件
pyridine
T=0°C; Inert atmosphere; Overall yield = 720 mg;
参考文献
ALMIRALL, S.A.; GRACIA FERRER, Jordi; CARRASCAL RIERA, Marta; ERRA SOLA, Montserrat
Patent: WO2014/60431 A1, 2014 ;
Location in patent: Page/Page column 85-86 ;
参考文献
Su, Weiguo; Zhang, Weihan; Yang, Haibin
Patent: US2013/190307 A1, 2013 ;
Location in patent: Paragraph 0158; 0161 ;
反应条件
1: With pyridine
T=20°C; 2 h;
2: With formic acid; ammonium acetate; water in acetonitrile
参考文献
GLAXO GROUP LIMITED; HAMBLIN, Julie, Nicole; JONES, Paul, Spencer; KEELING, Suzanne, Elaine; LE, Joelle; MITCHELL, Charlotte, Jane; PARR, Nigel, James
Patent: WO2010/125082 A1, 2010 ;
Location in patent: Page/Page column 75-76 ;
WO 2010/125082 A1
