7-氮杂双环[2,2,1]庚烷盐酸盐合成路线 （共 14 条）
反应条件
1: With lithium aluminium tetrahydride in tetrahydrofuran T=0 - 20°C; 98 h; 2: With hydrogenchloride in tetrahydrofuran
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2005/80402 A1, 2005 ;
Location in patent: Page/Page column 65 ;
WO 2005/080402 A1
反应条件
hydrogenchloride; Diethyloxytriphenylphosphorane in toluene T=68°C; 60 h; Title compound not separated from byproducts;
参考文献
Nelsen, Stephen F.; Ippoliti, J. Thomas; Frigo, Timothy B.; Petillo, Peter A.
Journal of the American Chemical Society, 1989 , vol. 111, # 5 p. 1776 - 1781
反应条件
hydrogenchloride in diethyl ether
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2004/18480 A1, 2004 ;
Location in patent: Page 88-89 ;
WO 2004/018480 A1
反应条件
hydrogenchloride in toluene T=68°C; 60 h; Yield given. Yields of byproduct given;
参考文献
Nelsen, Stephen F.; Ippoliti, J. Thomas; Frigo, Timothy B.; Petillo, Peter A.
Journal of the American Chemical Society, 1989 , vol. 111, # 5 p. 1776 - 1781
反应条件
1: With water; sodium hydroxide in dichloromethane T=25°C; 2: With hydrogenchloride in dichloromethane; water 0.5 h; Product distribution / selectivity;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; ZHANG, Beili; KRAWIEC, Mariusz; LUISI, Brian; MEDEK, Ales
Patent: WO2011/50220 A1, 2011 ;
Location in patent: Page/Page column 41 ;
WO 2011/050220 A1
反应条件
1: KOH; Et3N / acetonitrile 2: 80 percent / PPh3; DEAD / tetrahydrofuran / 25 °C 3: sodium naphthalide / 1,2-dimethoxy-ethane / -35 - 25 °C View Scheme
参考文献
Cheng, Jie; Trudell, Mark L.
Organic Letters, 2001 , vol. 3, # 9 p. 1371 - 1373
反应条件
1: 80 percent / PPh3; DEAD / tetrahydrofuran / 25 °C 2: sodium naphthalide / 1,2-dimethoxy-ethane / -35 - 25 °C View Scheme
参考文献
Cheng, Jie; Trudell, Mark L.
Organic Letters, 2001 , vol. 3, # 9 p. 1371 - 1373
反应条件
1.1: sodium carbonate / dichloromethane; water / 20 °C 2.1: triethylamine / tetrahydrofuran / 18 h / 0 - 17 °C 3.1: dichloromethane / 15 h / 20 °C / Inert atmosphere; Industry scale 4.1: sodium hydroxide; water / 25 °C 4.2: 0.5 h View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; ZHANG, Beili; KRAWIEC, Mariusz; LUISI, Brian; MEDEK, Ales
Patent: WO2011/50220 A1, 2011 ;
WO 2011/050220 A1
反应条件
1.1: triethylamine / tetrahydrofuran / 0 °C / Inert atmosphere 1.2: 3 h / 0 - 5 °C 2.1: dichloromethane / 20 °C / Inert atmosphere 3.1: sodium hydroxide; water / dichloromethane / 25 °C 3.2: 0.5 h View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; ZHANG, Beili; KRAWIEC, Mariusz; LUISI, Brian; MEDEK, Ales
Patent: WO2011/50220 A1, 2011 ;
WO 2011/050220 A1
反应条件
1.1: dichloromethane / 20 °C / Inert atmosphere 2.1: sodium hydroxide; water / dichloromethane / 25 °C 2.2: 0.5 h View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; ZHANG, Beili; KRAWIEC, Mariusz; LUISI, Brian; MEDEK, Ales
Patent: WO2011/50220 A1, 2011 ;
WO 2011/050220 A1
