2-氨基喹啉-6-甲酸苄酯合成路线 （共 9 条）
反应条件
ammonium chloride; triethylamine; p-toluenesulfonyl chloride in 1,2-dichloro-ethane
T=-10 - 25°C; 9 - 20 h; Product distribution / selectivity;
参考文献
PFIZER PRODUCTS INC.
Patent: WO2005/80373 A1, 2005 ;
Location in patent: Page/Page column 83 ;
反应条件
1: With phthalic anhydride; urea hydrogen peroxide addition compound in dichloromethane
T=23°C;
2: With p-toluenesulfonyl chloride in dichloromethane
3: With ammonium chloride; triethylamine
T=23°C;
参考文献
Robinson, Ralph P.; Bartlett, Jeremy A.; Bertinato, Peter; Bessire, Andrew J.; Cosgrove, Judith; Foley, Patrick M.; Manion, Tara B.; Minich, Martha L.; Ramos, Brenda; Reese, Matthew R.; Schmahai, Theodore J.; Swick, Andrew G.; Tess, David A.; Vaz, Alfin; Wolford, Angela
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 14 p. 4150 - 4154
反应条件
1.1: 1,1'-carbonyldiimidazole
1.2: 23 °C
2.1: phthalic anhydride; urea hydrogen peroxide addition compound / dichloromethane / 23 °C
2.3: 23 °C
View Scheme
参考文献
Robinson, Ralph P.; Bartlett, Jeremy A.; Bertinato, Peter; Bessire, Andrew J.; Cosgrove, Judith; Foley, Patrick M.; Manion, Tara B.; Minich, Martha L.; Ramos, Brenda; Reese, Matthew R.; Schmahai, Theodore J.; Swick, Andrew G.; Tess, David A.; Vaz, Alfin; Wolford, Angela
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 14 p. 4150 - 4154
反应条件
1.1: 1,1'-carbonyldiimidazole
1.2: 23 °C
2.1: phthalic anhydride; urea hydrogen peroxide addition compound / dichloromethane / 23 °C
2.3: 23 °C
View Scheme
参考文献
Robinson, Ralph P.; Bartlett, Jeremy A.; Bertinato, Peter; Bessire, Andrew J.; Cosgrove, Judith; Foley, Patrick M.; Manion, Tara B.; Minich, Martha L.; Ramos, Brenda; Reese, Matthew R.; Schmahai, Theodore J.; Swick, Andrew G.; Tess, David A.; Vaz, Alfin; Wolford, Angela
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 14 p. 4150 - 4154
反应条件
1.1: 1,1'-carbonyldiimidazole / ethyl acetate / 4 h / 20 - 25 °C / |Inert atmosphere; |Large scale
1.2: 12 h / 20 - 25 °C / |Inert atmosphere; |Large scale
2.1: urea hydrogen peroxide addition compound; phthalic anhydride / dichloromethane / 12 h / 20 - 25 °C / |Inert atmosphere
3.1: p-toluenesulfonyl chloride / dichloromethane / |Inert atmosphere
3.2: |Inert atmosphere
View Scheme
参考文献
Couturier, Michel; Le, Tung
Organic Process Research and Development, 2006 , vol. 10, # 3 p. 534 - 538
反应条件
1.1: urea hydrogen peroxide addition compound; phthalic anhydride / dichloromethane / 12 h / 20 - 25 °C / |Inert atmosphere
2.1: p-toluenesulfonyl chloride / dichloromethane / |Inert atmosphere
2.2: |Inert atmosphere
View Scheme
参考文献
Couturier, Michel; Le, Tung
Organic Process Research and Development, 2006 , vol. 10, # 3 p. 534 - 538
反应条件
1: With p-toluenesulfonyl chloride in dichloromethane
Inert atmosphere;
2: With hydroxylamine hydrochloride in dichloromethane
Inert atmosphere; Overall yield = 40 percent;
参考文献
Couturier, Michel; Le, Tung
Organic Process Research and Development, 2006 , vol. 10, # 3 p. 534 - 538
反应条件
1.1: 1,1'-carbonyldiimidazole / ethyl acetate / 4 h / 20 - 25 °C / |Inert atmosphere; |Large scale
1.2: 12 h / 20 - 25 °C / |Inert atmosphere; |Large scale
2.1: urea hydrogen peroxide addition compound; phthalic anhydride / dichloromethane / 12 h / 20 - 25 °C / |Inert atmosphere
3.1: p-toluenesulfonyl chloride / dichloromethane / |Inert atmosphere
3.2: |Inert atmosphere
View Scheme
参考文献
Couturier, Michel; Le, Tung
Organic Process Research and Development, 2006 , vol. 10, # 3 p. 534 - 538
反应条件
ammonia; p-toluenesulfonyl chloride in dichloromethane
Inert atmosphere;
参考文献
Couturier, Michel; Le, Tung
Organic Process Research and Development, 2006 , vol. 10, # 3 p. 534 - 538
