6-溴-3,4-二氢-2H-吡啶并[3,2-b][1,4]噁嗪合成路线 （共 6 条）
反应条件
1: With borane-THF in tetrahydrofuran
T=90°C; 1.5 h;
2: With methanol in tetrahydrofuran
T=90°C; 0.333333 h;
参考文献
Shionogi and Co., Ltd.
Patent: EP2341052 A1, 2011 ;
Location in patent: Page/Page column 35; 36 ;
反应条件
1: With iron; acetic acid
T=90°C; 5 h;
2: With potassium carbonate in N,N-dimethyl-formamide
T=70 - 90°C;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2007/141473 A1, 2007 ;
Location in patent: Page/Page column 268; 269 ;
WO 2007/141473 A1
反应条件
potassium carbonate in N,N-dimethyl-formamide
T=90°C;
参考文献
SIRTRIS PHARMACEUTICALS, INC.; NG, Pui, Yee; BLUM, Charles; MCPHERSON, Lauren; PERNI, Robert, B.; VU, Chi, B.; AHMED, Mohammed, Mahmood; DISCH, Jeremy, S.
Patent: WO2011/59839 A1, 2011 ;
Location in patent: Page/Page column 65 ;
WO 2011/059839 A1
反应条件
1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 2 h / 0 - 20 °C
2: acetic acid; iron / 5 h / 90 °C
3: potassium carbonate / N,N-dimethyl-formamide / 90 °C
View Scheme
参考文献
SIRTRIS PHARMACEUTICALS, INC.; NG, Pui, Yee; BLUM, Charles; MCPHERSON, Lauren; PERNI, Robert, B.; VU, Chi, B.; AHMED, Mohammed, Mahmood; DISCH, Jeremy, S.
Patent: WO2011/59839 A1, 2011 ;
WO 2011/059839 A1
反应条件
1.1: sodium methylate; bromine / methanol / 0.5 h / 0 °C
1.2: 0.17 h / 0 °C
2.1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 2 h / 0 - 20 °C
3.1: acetic acid; iron / 5 h / 90 °C
4.1: potassium carbonate / N,N-dimethyl-formamide / 90 °C
View Scheme
参考文献
SIRTRIS PHARMACEUTICALS, INC.; NG, Pui, Yee; BLUM, Charles; MCPHERSON, Lauren; PERNI, Robert, B.; VU, Chi, B.; AHMED, Mohammed, Mahmood; DISCH, Jeremy, S.
Patent: WO2011/59839 A1, 2011 ;
WO 2011/059839 A1
反应条件
1.1: acetic acid; iron / 2 h / 100 °C
2.1: borane-THF / tetrahydrofuran / 1.5 h / 90 °C
2.2: 0.33 h / 90 °C
View Scheme
参考文献
Shionogi and Co., Ltd.
Patent: EP2341052 A1, 2011 ;
