3,5-二氟吡啶-2-羧酸合成路线 (共 5 条)
反应条件
sulfuric acid; water T=110°C; 22 h;
参考文献
EP2305672 A1, ;
Page/Page column 79 ;
反应条件
thionyl chloride T=60°C; 3 h; Cooling with ice;
参考文献
CONFLUENCE LIFE SCIENCES, INC.; SELNESS, Shaun R.; Devadas, Balekudru; Hockerman, Susan L.; Monahan, Joseph B.
Patent: US2013/143906 A1, 2013 ;
Location in patent: Paragraph 0315 ;
反应条件
1: With thionyl chloride T=0 - 20°C; 72.5 h; 2: With sodium hydrogencarbonate in water
参考文献
Astellas Pharma Inc.
Patent: EP2085383 A1, 2009 ;
Location in patent: Page/Page column 26 ;
EP 2085383 A1
反应条件
1.1: p-toluenesulfonyl chloride / pyridine / 1 h / 0 °C 1.2: 0.25 h 2.1: methanol / 1.5 h / 25 °C View Scheme
参考文献
MERCK SHARP and DOHME CORP.; CUMMING, Jared, N.; GILBERT, Eric, J.; STAMFORD, Andrew, W.
Patent: WO2012/138734 A1, 2012 ;
WO 2012/138734 A1
反应条件
1: 3,5-difluoropyridine-2-carboxylic acid With hydrogenchloride; oxalyl dichloride; N,N-dimethyl-formamide in 1,4-dioxane; dichloromethane
T=20°C; 2 h;
2: 2-methylamino-ethanol With triethylamine in dichloromethane
T=20°C; 20 h;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2007/7040 A1, 2007 ;
Location in patent: Page/Page column 65-66 ;
WO 2007/007040 A1