8-氯咪唑并[1,2-a]吡嗪合成路线 （共 9 条）
反应条件
1: 2-bromoacetaldehyde diethyl acetal With hydrogen bromide in water 1 h; Reflux; 2: 3-amino-2-chloropyrazine With hydrogen bromide in ethylene glycol dimethyl ether; water 3 h; Reflux;
参考文献
Oncotherapy Science, Inc.
Patent: US2012/59162 A1, 2012 ;
Location in patent: Page/Page column 38-39 ;
反应条件
potassium carbonate in tetrahydrofuran; water T=20°C; 9 h; Reflux;
参考文献
BAYER PHARMA AKTIENGESELLSCHAFT; KOPPITZ, Marcus; KLAR, Ulrich; JAUTELAT, Rolf; KOSEMUND, Dirk; BOHLMANN, Rolf; BADER, Benjamin; LIENAU, Philip; SIEMEISTER, Gerhard
Patent: WO2012/80229 A1, 2012 ;
Location in patent: Page/Page column 39-40 ;
WO 2012/080229 A1
反应条件
1: 2-bromoacetaldehyde diethyl acetal With hydrogen bromide in water T=95°C; 1.5 h; 2: With sodium hydrogencarbonate in isopropyl alcohol 0.5 h; 3: 3-amino-2-chloropyrazine With hydrogen bromide more than 3 stages;
参考文献
MERCK SHARP and DOHME LIMITED
Patent: WO2004/41826 A1, 2004 ;
Location in patent: Page 26 ;
反应条件
1: in water; isopropyl alcohol 2 h; Heating / reflux; 2: With sodium hydrogencarbonate in dichloromethane; water
参考文献
WO2009/24585 A2, ;
Page/Page column 46 ;
反应条件
hydrogen bromide in ethylene glycol dimethyl ether 1 h; Heating / reflux;
参考文献
US2007/105864 A1, ;
Page/Page column 121 ;
US 20070105864 A1
反应条件
hydrogenchloride in ethylene glycol dimethyl ether Reflux;
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 20, # 17 p. 5170 - 5174
反应条件
N-bromosuccinmide in dichloromethane T=20°C; 2 h;
参考文献
BIOFOCUS DPI LIMITED
Patent: WO2009/24585 A2, 2009 ;
Location in patent: Page/Page column 46 ;
反应条件
bromine; acetic acid T=20°C; 16 h;
参考文献
Janssen Pharmaceutica NV
Patent: US2012/329792 A1, 2012 ;
Location in patent: Page/Page column 36 ;
反应条件
1: dimethyl sulfoxide / 1 h / 85 °C
2: sodium acetate; bromine; potassium bromide / methanol / 1 h / 0 °C
View Scheme
参考文献
BAYER PHARMA AKTIENGESELLSCHAFT; KOPPITZ, Marcus; KLAR, Ulrich; JAUTELAT, Rolf; KOSEMUND, Dirk; BOHLMANN, Rolf; BADER, Benjamin; LIENAU, Philip; SIEMEISTER, Gerhard
Patent: WO2012/80229 A1, 2012 ;
WO 2012/080229 A1
