1-[6-(三氟甲基)-3-吡啶]乙酮合成路线 （共 8 条）
反应条件
in tetrahydrofuran; toluene T=0°C; 1 h;
参考文献
ELI LILLY AND COMPANY
Patent: US2012/302608 A1, 2012 ;
Location in patent: Page/Page column 12 ;
反应条件
1: malonic acid dimethyl ester With triethylamine; magnesium chloride in toluene 2.5 h; light cooling; 2: 6-(trifluoromethyl)pyridine-3-carbonyl chloride in toluene 2 h; Cooling; 3: With hydrogenchloride; water more than 3 stages;
参考文献
F. HOFFMANN-LA ROCHE AG
Patent: WO2008/34579 A1, 2008 ;
Location in patent: Page/Page column 24-25 ;
反应条件
1: in diethyl ether 2.5 h; 2: With hydrogenchloride; water in diethyl ether
参考文献
US2006/89370 A1, ;
Page/Page column 34 ;
反应条件
sec.-butyllithium in diethyl ether T=-78 - 20°C; 17 h;
参考文献
Dalence-Guzman, Maria F.; Toftered, Joergen; Oltner, Viveca Thornqvist; Wensbo, David; Johansson, Martin H.
Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 17 p. 4999 - 5003
反应条件
1.1: pyridine / dichloromethane / 20 °C 1.2: 1 h 2.1: toluene; tetrahydrofuran / 0 °C / Inert atmosphere View Scheme
参考文献
WO2008/123963 A1, ;
WO 2008/123963 A1
反应条件
1: (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 60 h 2: diethyl ether; tetrahydrofuran / 16 h View Scheme
反应条件
1.1: titanium tetraethoxide / tetrahydrofuran / Inert atmosphere; Reflux 1.2: -50 - 20 °C 1.3: 0 °C 2.1: hydrogenchloride / 1,4-dioxane; water / 2 h / 20 °C 2.2: pH 12 View Scheme
参考文献
RENOVIS, INC.
Patent: WO2008/123963 A1, 2008 ;
WO 2008/123963 A1
反应条件
1.1: titanium tetraethoxide / tetrahydrofuran / Inert atmosphere; Reflux
1.2: -50 - 20 °C
1.3: 0 °C
2.1: hydrogenchloride / 1,4-dioxane; water / 1.5 h / 20 °C
View Scheme
参考文献
RENOVIS, INC.
Patent: WO2008/123963 A1, 2008 ;
WO 2008/123963 A1
