2-溴-5-氟-4-硝基苯胺合成路线 （共 7 条）
反应条件
1.1: Zn(ClO4)2-2H2O / toluene / 20 - 80 °C / Molecular sieve 1.2: 30 °C / 750.08 Torr 2.1: sodium hydrogencarbonate / ethyl acetate 2.2: 20 °C 2.3: 80 °C / Inert atmosphere 3.1: dichloro bis(acetonitrile) palladium(II) / acetonitrile / 20 - 80 °C / Inert atmosphere View Scheme
参考文献
WO2011/119984 A1, ;
WO 2011/119984 A1
反应条件
triethylamine; bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide T=20 - 80°C;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; RUAH, Sara, Hadida, S.; GROOTENHUIS, Peter, D., J.; VAN GOOR, Fredrick; MILLER, Mark, T.; MCCARTNEY, Jason; ZHOU, Jinglan; BEAR, Brian; NUMA, Mehdi, Michel, Djamel
Patent: WO2010/53471 A1, 2010 ;
Location in patent: Page/Page column 60-61 ;
反应条件
1: With bromine; acetic acid in chloroform
T=0 - 20°C; 2 h;
2: With sodium hydroxide in chloroform; water
T=0°C; pH=8.0 - 9.0;
参考文献
Vertex Pharmaceuticals Incorported
Patent: US2011/98311 A1, 2011 ;
反应条件
in N2; water; ethyl acetate; isopropyl alcohol
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: US2012/15999 A1, 2012 ;
US 20120015999 A1
反应条件
1.1: Zn(ClO4)2-2H2O / toluene / 20 - 80 °C / Molecular sieve
1.2: 30 °C / 750.08 Torr
2.1: sodium hydrogencarbonate / ethyl acetate
2.2: 20 °C
2.3: 80 °C / Inert atmosphere
3.1: dichloro bis(acetonitrile) palladium(II) / acetonitrile / 20 - 80 °C / Inert atmosphere
4.1: triethylamine / dichloromethane / 0 - 20 °C
5.1: hydrogen / 5 palladium on charcoal / tetrahydrofuran / 96 h / 50 °C / 2250.23 - 3000.3 Torr / autoclave; Inert atmosphere
View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; LOOKER, ADAM; Littler, Benjamin Joseph; Choudhury, Anusuya; Harrison, Cristian; Veluri, Ravikanth; Ryan, Michael P.; Jiang, Licong; Luss-Lusis, Eduard
Patent: US2013/116238 A1, 2013 ;
反应条件
1: CuI; triethylamine / Pd(PPh3)2Cl2 / water; toluene
2: triethylamine / dichloromethane
3: tetrabutyl ammonium fluoride / N,N-dimethyl-formamide
View Scheme
参考文献
Vertex Pharmaceuticals Incorported
Patent: US2011/98311 A1, 2011 ;
反应条件
1: CuI; triethylamine / Pd(PPh3)2Cl2 / water; toluene
2: triethylamine / dichloromethane
3: potassium tert-butylate / N,N-dimethyl-formamide
View Scheme
参考文献
Vertex Pharmaceuticals Incorported
Patent: US2011/98311 A1, 2011 ;
