1-(4-氟苯基氨基甲酰基)环丙烷羧酸合成路线 （共 13 条）
反应条件
1: cyclopropane-1,1-dicarboxylic acid With thionyl chloride in isopropanol acetate T=25°C; 5 h; Large scale; 2: 4-fluoroaniline With triethylamine in isopropanol acetate 1 h; Large scale;
参考文献
EXELIXIS, INC.; AFTAB, Dana, T; SCHIMMOLLER, Frauke
Patent: WO2013/70890 A1, 2013 ;
Location in patent: Paragraph 00114-00116 ;
反应条件
1: With water; lithium hydroxide hydrate in tetrahydrofuran T=20°C; 0.5 h; 2: With hydrogenchloride pH=5; Cooling with ice;
参考文献
DECIPHERA PHARMACEUTICALS, LLC; FLYNN, Daniel L.; KAUFMAN, Michael D.
Patent: WO2011/137342 A1, 2011 ;
Location in patent: Page/Page column 34 ;
WO 2011/137342 A1
反应条件
potassium hydroxide in tetrahydrofuran; ethanol
参考文献
Xi, Ning
Patent: US2010/239576 A1, 2010 ;
US 20100239576 A1
反应条件
in tetrahydrofuran T=0°C; 1.5 h; Inert atmosphere;
参考文献
Chen, Danqi; Wang, Ying; Ma, Yuchi; Xiong, Bing; Ai, Jing; Chen, Yi; Geng, Meiyu; Shen, Jingkang
ChemMedChem, 2012 , vol. 7, # 6 p. 1057 - 1070
反应条件
1.1: N-ethyl-N,N-diisopropylamine; O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate / N,N-dimethyl-formamide / 15 h / 20 °C 2.1: water; lithium hydroxide hydrate / tetrahydrofuran / 0.5 h / 20 °C 2.2: pH 5 / Cooling with ice View Scheme
参考文献
WO2011/137342 A1, ;
WO 2011/137342 A1
反应条件
1.1: N-ethyl-N,N-diisopropylamine; O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate / N,N-dimethyl-formamide / 15 h / 20 °C 2.1: water; lithium hydroxide hydrate / tetrahydrofuran / 0.5 h / 20 °C 2.2: pH 5 / Cooling with ice View Scheme
参考文献
WO2011/137342 A1, ;
WO 2011/137342 A1
反应条件
1.1: triethylamine / tetrahydrofuran / 0.5 h / 0 °C / Inert atmosphere 1.2: 0.5 h / 0 °C / Inert atmosphere 2.1: tetrahydrofuran / 1.5 h / 0 °C / Inert atmosphere View Scheme
参考文献
ChemMedChem, , vol. 7, # 6 p. 1057 - 1070
反应条件
1: sodium hydroxide / ethanol; water / 0 - 20 °C 2: thionyl chloride / 2 h / |Reflux 3: triethylamine / dichloromethane / 0 - 20 °C 4: sodium hydroxide / ethanol / 1 h / 65 °C View Scheme
反应条件
1: thionyl chloride / 2 h / |Reflux 2: triethylamine / dichloromethane / 0 - 20 °C 3: sodium hydroxide / ethanol / 1 h / 65 °C View Scheme
反应条件
1: 1-((4-fluorophenyl)carbamoyl)cyclopropanecarboxylic acid With oxalyl dichloride; N,N-dimethyl-formamide in tetrahydrofuran T=15 - 20°C; Industry scale; 2: 3-fluoro-4-[6-methoxy-7-(3-morpholin-4-yl-propoxy)-quinolin-4-yloxy]-phenylamine With potassium carbonate in tetrahydrofuran T=15 - 20°C; 3 h; Industry scale;
参考文献
WO2011/9095 A1, ;
Page/Page column 18-20 ;
WO 2011/009095 A1
