N-[4-[2-(2-氨基-4,7-二氢-4-氧代-1H-吡咯并[2,3-d]嘧啶-5-基)乙基]苯甲酰]-L-谷氨酸二乙酯对甲苯磺酸盐合成路线 （共 8 条）
反应条件
1: 2-chloro-4,6-dimethoxy-[1,3,5]triazine; 4-methylmorpholine N-oxide / N,N-dimethyl-formamide / 1.5 h / 25 °C / |Large scale 2: ethanol / 3 h / |Reflux; |Large scale View Scheme
参考文献
Organic Process Research and Development, , vol. 3, # 3 p. 184 - 188
反应条件
1: DBBA; hydrogen bromide; acetic acid / dichloromethane / 25 °C / |Large scale 2: sodium acetate / water; acetonitrile / 3 h / 40 °C / |Large scale 3: sodium hydroxide / water / 1.5 h / 40 °C / |Large scale 4: 2-chloro-4,6-dimethoxy-[1,3,5]triazine; 4-methylmorpholine N-oxide / N,N-dimethyl-formamide / 1.5 h / 25 °C / |Large scale 5: ethanol / 3 h / |Reflux; |Large scale View Scheme
参考文献
Organic Process Research and Development, , vol. 3, # 3 p. 184 - 188
反应条件
1: hydrogen; 5 palladium on charcoal / dichloromethane / 3.5 h / 3345.86 Torr / |Inert atmosphere; |Autoclave; |Large scale 2: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; potassium bromide; sodium hypochlorite; sodium hydrogencarbonate / dichloromethane; water / -10 - 20 °C / pH 9.5 / |Large scale 3: DBBA; hydrogen bromide; acetic acid / dichloromethane / 25 °C / |Large scale 4: sodium acetate / water; acetonitrile / 3 h / 40 °C / |Large scale 5: sodium hydroxide / water / 1.5 h / 40 °C / |Large scale 6: 2-chloro-4,6-dimethoxy-[1,3,5]triazine; 4-methylmorpholine N-oxide / N,N-dimethyl-formamide / 1.5 h / 25 °C / |Large scale 7: ethanol / 3 h / |Reflux; |Large scale View Scheme
参考文献
Organic Process Research and Development, , vol. 3, # 3 p. 184 - 188
反应条件
1: palladium dichloride; triphenylphosphine; copper(l) iodide; diethylamine / ethyl acetate / 4 h / 50 °C / |Large scale 2: hydrogen; 5 palladium on charcoal / dichloromethane / 3.5 h / 3345.86 Torr / |Inert atmosphere; |Autoclave; |Large scale 3: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; potassium bromide; sodium hypochlorite; sodium hydrogencarbonate / dichloromethane; water / -10 - 20 °C / pH 9.5 / |Large scale 4: DBBA; hydrogen bromide; acetic acid / dichloromethane / 25 °C / |Large scale 5: sodium acetate / water; acetonitrile / 3 h / 40 °C / |Large scale 6: sodium hydroxide / water / 1.5 h / 40 °C / |Large scale 7: 2-chloro-4,6-dimethoxy-[1,3,5]triazine; 4-methylmorpholine N-oxide / N,N-dimethyl-formamide / 1.5 h / 25 °C / |Large scale 8: ethanol / 3 h / |Reflux; |Large scale View Scheme
参考文献
Organic Process Research and Development, , vol. 3, # 3 p. 184 - 188
反应条件
1: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; potassium bromide; sodium hypochlorite; sodium hydrogencarbonate / dichloromethane; water / -10 - 20 °C / pH 9.5 / |Large scale 2: DBBA; hydrogen bromide; acetic acid / dichloromethane / 25 °C / |Large scale 3: sodium acetate / water; acetonitrile / 3 h / 40 °C / |Large scale 4: sodium hydroxide / water / 1.5 h / 40 °C / |Large scale 5: 2-chloro-4,6-dimethoxy-[1,3,5]triazine; 4-methylmorpholine N-oxide / N,N-dimethyl-formamide / 1.5 h / 25 °C / |Large scale 6: ethanol / 3 h / |Reflux; |Large scale View Scheme
参考文献
Organic Process Research and Development, , vol. 3, # 3 p. 184 - 188
反应条件
in ethanol 3 h; RefluxLarge scale;
参考文献
Barnett, Charles J.; Wilson, Thomas M.; Kobierski, Michael E.
Organic Process Research and Development, 1999 , vol. 3, # 3 p. 184 - 188
反应条件
1: 1 h / 20 - 25 °C 2: ethanol View Scheme
参考文献
Organic Process Research and Development, , vol. 9, # 6 p. 738 - 742
反应条件
1: With sodium hydroxide; water T=2°C; 1.5 h; 2: With hydrogenchloride in water T=2 - 70°C; pH=3.9 - 4.1; 4.83333 h;
参考文献
Busolli, Jonathan; Diulgheroff, Nicola; Nemethne Racz, Csilla; Pirkes, Moran; Pontiroli, Alessandro; Villa, Marco; Aronhime, Judith
Patent: US2008/45711 A1, 2008 ;
Location in patent: Page/Page column 11 ;
