3',4',5'-三氟联苯基-2-胺合成路线 （共 11 条）
反应条件
1: (3,4,5-trifluorophenyl)magnesium bromide With zinc(II) chloride in tetrahydrofuran; 1-methyl-pyrrolidin-2-one
T=30°C; 0.166667 h;
2: RR 265 With PEPPSI™-IPr catalyst in tetrahydrofuran; 1-methyl-pyrrolidin-2-one
T=25 - 50°C; 6 h;
参考文献
BASF SE
Patent: US2011/301356 A1, 2011 ;
Location in patent: Page/Page column 10 ;
反应条件
1: (3,4,5-trifluorophenyl)magnesium bromide With zinc(II) chloride in tetrahydrofuran
T=25°C; 0.5 h;
2: 2-chloro-aniline With PEPPSI™-IPr catalyst in tetrahydrofuran; 1-methyl-pyrrolidin-2-one
T=25°C; 6.5 h; Reflux;
参考文献
BASF SE
Patent: US2011/301356 A1, 2011 ;
Location in patent: Page/Page column 9 ;
反应条件
1: (3,4,5-trifluorophenyl)magnesium bromide With zinc(II) chloride in tetrahydrofuran; toluene
T=25°C; 0.333333 h;
2: 1-Bromo-2-aminobenzene With bis(dibenzylideneacetone)-palladium(0); [(t-Bu)3PH]BF4 in tetrahydrofuran; 1-methyl-pyrrolidin-2-one; toluene
T=25°C; 5 h;
参考文献
BASF SE
Patent: US2011/301356 A1, 2011 ;
Location in patent: Page/Page column 9 ;
反应条件
water; butan-1-ol; sulfuric acid
Reflux;
参考文献
BASF SE
Patent: US2011/301356 A1, 2011 ;
Location in patent: Page/Page column 10 ;
反应条件
bis-triphenylphosphine-palladium(II) chloride; potassium carbonate in 1,4-dioxane; water
T=70°C; 3 h; Inert atmosphere;
参考文献
Maleckis, Ansis; Kampf, Jeff W.; Sanford, Melanie S.
Journal of the American Chemical Society, 2013 , vol. 135, # 17 p. 6618 - 6625
反应条件
manganese(IV) oxide in acetonitrile
T=20°C; Overall yield = 75 percent; regioselective reaction;
参考文献
Jasch, Hannelore; Scheumann, Julia; Heinrich, Markus R.
Journal of Organic Chemistry, 2012 , vol. 77, # 23 p. 10699 - 10706
反应条件
1.1: ethanol / 8 h / Reflux
2.1: zinc(II) chloride / 1-methyl-pyrrolidin-2-one; tetrahydrofuran / 0.17 h / 30 °C
2.2: 6 h / 25 - 50 °C
View Scheme
参考文献
BASF SE
Patent: US2011/301356 A1, 2011 ;
反应条件
1.1: magnesium / tetrahydrofuran / 7 h / 25 - 35 °C / Inert atmosphere
2.1: zinc(II) chloride / toluene; tetrahydrofuran / 0.33 h / 25 °C
2.2: 5 h / 25 °C
View Scheme
参考文献
BASF SE
Patent: US2011/301356 A1, 2011 ;
反应条件
dCypp; 1,8-diazabicyclo[5.4.0]undec-7-ene; bis(benzonitrile)palladium(II) dichloride in N,N-dimethyl-formamide
T=130°C; P=11251.1 Torr; 16 h; Inert atmosphere; Product distribution / selectivity;
参考文献
BASF SE
Patent: US2010/174094 A1, 2010 ;
Location in patent: Page/Page column 11 ;
反应条件
potassium tert-butylate in tetrahydrofuran
T=0 - 20°C;
参考文献
Moradi, Wahed Ahmed; Lui, Norbert; Dockner, Michael
Patent: US2014/128617 A1, 2014 ;
Location in patent: Paragraph 0094; 0095 ;
