N-(4-(2-(2-氨基-4-氧代-4,7-二氢-3H-吡咯并[2,3-d]嘧啶-5-基)乙基)苯甲酰基)-L-谷氨酸二乙酯合成路线 (共 29 条)
反应条件
1: 91 percent / ethyl acetate; H2O / 24 h / 50 °C 2: 57 percent 3: 62 percent / 4-methylmorpholine; 2-chloro-4,6-dimethoxy-1,3,5-triazine / 20 °C View Scheme
参考文献
Tetrahedron Letters, , vol. 40, # 21 p. 4023 - 4026
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 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 View Scheme
参考文献
Organic Process Research and Development, , vol. 3, # 3 p. 184 - 188
反应条件
1: 5,5-dibromomeldrum's acid; hydrogenchloride / diethyl ether / 24 h / 20 °C 2: sodium acetate / water; methanol / 3 h / 45 °C 3: sodium hydroxide / methanol / 24 h / 40 - 50 °C / |Inert atmosphere 4: 2-chloro-4,6-dimethoxy-[1,3,5]triazine; 4-methyl-morpholine / N,N-dimethyl-formamide / 6 h / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 56, # 24 p. 10016 - 10032
反应条件
1: sodium acetate / water; methanol / 3 h / 45 °C 2: sodium hydroxide / methanol / 24 h / 40 - 50 °C / |Inert atmosphere 3: 2-chloro-4,6-dimethoxy-[1,3,5]triazine; 4-methyl-morpholine / N,N-dimethyl-formamide / 6 h / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 56, # 24 p. 10016 - 10032
反应条件
1: sodium hydroxide / methanol / 24 h / 40 - 50 °C / |Inert atmosphere 2: 2-chloro-4,6-dimethoxy-[1,3,5]triazine; 4-methyl-morpholine / N,N-dimethyl-formamide / 6 h / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 56, # 24 p. 10016 - 10032
参考文献
Organic Process Research and Development, , vol. 9, # 6 p. 738 - 742
反应条件
2: 1 h / 20 - 25 °C View Scheme
参考文献
Organic Process Research and Development, , vol. 9, # 6 p. 738 - 742
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