甲氨蝶呤alpha-天冬氨酸合成路线 (共 7 条)
反应条件
1: 68 percent / (i-Pr)2NEt / dioxane; H2O
2: Et3N / dimethylformamide; dioxane / 1 h / -10 °C
3: Et3N / dimethylformamide; dioxane / 2 h / 25 °C
4: H2 / 5percent Pd/C / dioxane / 20 h / Ambient temperature
5: N,N-dimethyl-acetamide / 120 h / 25 °C
View Scheme
参考文献
Piper; Montgomery; Sirotnak; Chello
Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 182 - 187
反应条件
1: 86 percent / 2 N NaOH / dioxane; H2O / 0.5 h / 0 - 5 °C
2: 99 percent / SOCl2 / benzene / 2 h / Heating
3: 68 percent / (i-Pr)2NEt / dioxane; H2O
4: Et3N / dimethylformamide; dioxane / 1 h / -10 °C
5: Et3N / dimethylformamide; dioxane / 2 h / 25 °C
6: H2 / 5percent Pd/C / dioxane / 20 h / Ambient temperature
7: N,N-dimethyl-acetamide / 120 h / 25 °C
View Scheme
参考文献
Piper; Montgomery; Sirotnak; Chello
Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 182 - 187
反应条件
1: 99 percent / SOCl2 / benzene / 2 h / Heating
2: 68 percent / (i-Pr)2NEt / dioxane; H2O
3: Et3N / dimethylformamide; dioxane / 1 h / -10 °C
4: Et3N / dimethylformamide; dioxane / 2 h / 25 °C
5: H2 / 5percent Pd/C / dioxane / 20 h / Ambient temperature
6: N,N-dimethyl-acetamide / 120 h / 25 °C
View Scheme
参考文献
Piper; Montgomery; Sirotnak; Chello
Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 182 - 187
反应条件
1: 68 percent / (i-Pr)2NEt / dioxane; H2O
2: Et3N / dimethylformamide; dioxane / 1 h / -10 °C
3: Et3N / dimethylformamide; dioxane / 2 h / 25 °C
4: H2 / 5percent Pd/C / dioxane / 20 h / Ambient temperature
5: N,N-dimethyl-acetamide / 120 h / 25 °C
View Scheme
参考文献
Piper; Montgomery; Sirotnak; Chello
Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 182 - 187
反应条件
1: Et3N / dimethylformamide; dioxane / 1 h / -10 °C
2: Et3N / dimethylformamide; dioxane / 2 h / 25 °C
3: H2 / 5percent Pd/C / dioxane / 20 h / Ambient temperature
4: N,N-dimethyl-acetamide / 120 h / 25 °C
View Scheme
参考文献
Piper; Montgomery; Sirotnak; Chello
Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 182 - 187
反应条件
1: H2 / 5percent Pd/C / dioxane / 20 h / Ambient temperature
2: N,N-dimethyl-acetamide / 120 h / 25 °C
View Scheme
参考文献
Piper; Montgomery; Sirotnak; Chello
Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 182 - 187
反应条件
in N,N-dimethyl acetamide
T=25°C; 120 h; Yield given;
参考文献
Piper; Montgomery; Sirotnak; Chello
Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 182 - 187