2-溴-4-氟-6-甲基苯胺合成路线 （共 5 条）
反应条件
N-bromosuccinmide in N,N-dimethyl-formamide T=20°C;
参考文献
WO2011/6803 A1, ;
Page/Page column 34 ;
WO 2011/006803 A1
反应条件
1: With hydrogenchloride; copper(l) chloride in water; toluene T=0°C; Heating; 2: With Na2CO3*10H2O; sodium nitrite in water; toluene T=2 - 70°C; pH=7;
参考文献
NERVIANO MEDICAL SCIENCES S.R.L.; PAPEO, Gianluca Mariano Enrico; ANATOLIEVNA BUSEL, Alina; CASALE, Elena; KHVAT, Alexander; KRASAVIN, Mikhail Yurievitch; ORSINI, Paolo; POSTERI, Helena; SCOLARO, Alessandra
Patent: WO2011/6803 A1, 2011 ;
Location in patent: Page/Page column 34-35 ;
WO 2011/006803 A1
反应条件
1: 2-bromo-4-fluoro-6-methylphenylamine With hydrogenchloride in water T=2°C; 2: With sodium carbonate; sodium nitrite in water T=5°C; pH=Ca. 7; 3: cyanocuprate in water T=5 - 70°C;
参考文献
NERVIANO MEDICAL SCIENCES S.R.L.; PAPEO, Gianluca Mariano Enrico; KRASAVIN, Mikhail Yurievitch; ORSINI, Paolo; SCOLARO, Alessandra
Patent: WO2014/64149 A1, 2014 ;
Location in patent: Page/Page column 27; 28 ;
反应条件
1.1: hydrogenchloride; copper(l) chloride / toluene; water / 0 °C / Heating 1.2: 2 - 70 °C / pH 7 2.1: sulfuric acid / water / 15 h / 150 °C 3.1: sodium nitrite; sulfuric acid / water / 80 °C View Scheme
参考文献
NERVIANO MEDICAL SCIENCES S.R.L.; PAPEO, Gianluca Mariano Enrico; KRASAVIN, Mikhail Yurievitch; ORSINI, Paolo; SCOLARO, Alessandra
Patent: WO2014/64149 A1, 2014 ;
反应条件
1.1: hydrogenchloride / water / 2 °C
1.2: 5 °C / pH Ca. 7
1.3: 5 - 70 °C
2.1: sulfuric acid / water / 150 °C
3.1: sodium nitrite; sulfuric acid / water / 1 h / 80 °C
3.2: 20 °C
4.1: potassium carbonate / N,N-dimethyl-formamide / 23 h / 20 °C
5.1: sodium carbonate; palladium diacetate / 1-methyl-pyrrolidin-2-one / 120 °C / |Inert atmosphere; |Sealed tube
View Scheme
参考文献
NERVIANO MEDICAL SCIENCES S.R.L.; PAPEO, Gianluca Mariano Enrico; KRASAVIN, Mikhail Yurievitch; ORSINI, Paolo; SCOLARO, Alessandra
Patent: WO2014/64149 A1, 2014 ;
