N-(5-甲氨基-2-噻吩甲酰基)-L-谷氨酸二乙酯合成路线 (共 15 条)
反应条件
trifluoroacetic acid in dichloromethane T=20°C; 1 h;
参考文献
Cao, Sheng-Li; Wan, Rong; Feng, Yu-Ping
Synthetic Communications, 2003 , vol. 33, # 20 p. 3519 - 3526
反应条件
2,6-dimethylpyridine in N,N-dimethyl-formamide; toluene T=70°C; 24 h;
参考文献
Marsham, Peter R.; Hughes, Leslie R.; Jackman, Ann L.; Hayter, Anthony J.; Oldfield, John; et al.
Journal of Medicinal Chemistry, 1991 , vol. 34, # 5 p. 1594 - 1605
反应条件
in EtOAc-cyclohexane; N,N-dimethyl-formamide
参考文献
SRI International; Sloan-Kettering Institute
Patent: US5536724 A1, 1996 ;
反应条件
1: 84 percent / 1.) Et3N / CH2Cl2 / 1.) 5 deg C, 1 h, 2.) 20 deg C, 1 h 2: 82 percent / activated Fe, FeSO4*7H2O / methanol; H2O / 5 h / 70 °C 3: 48 percent / 2,6-lutidine / dimethylformamide; toluene / 24 h / 70 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 5 p. 1594 - 1605
反应条件
1: 84 percent / 1.) Et3N / CH2Cl2 / 1.) 5 deg C, 1 h, 2.) 20 deg C, 1 h 2: 82 percent / activated Fe, FeSO4*7H2O / methanol; H2O / 5 h / 70 °C 3: 48 percent / 2,6-lutidine / dimethylformamide; toluene / 24 h / 70 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 5 p. 1594 - 1605
反应条件
1: 1.) LDA / 1.) THF, hexane, -78 deg C, 30 min, 2.) from -50 deg C to 20 deg C, overnight 2: oxalyl chloride / dimethylformamide; CH2Cl2 / 0.5 h 3: Et3N / CH2Cl2 / 10 - 15 °C 4: 58 percent / CF3CO2HF / 16 h / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 5 p. 1594 - 1605
反应条件
1: oxalyl chloride / dimethylformamide; CH2Cl2 / 0.5 h 2: Et3N / CH2Cl2 / 10 - 15 °C 3: 58 percent / CF3CO2HF / 16 h / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 5 p. 1594 - 1605
反应条件
1: 82 percent / activated Fe, FeSO4*7H2O / methanol; H2O / 5 h / 70 °C 2: 48 percent / 2,6-lutidine / dimethylformamide; toluene / 24 h / 70 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 5 p. 1594 - 1605
反应条件
N-ethyl-N,N-diisopropylamine in N,N-dimethyl-formamide 44 h;
参考文献
Journal of Medicinal Chemistry, , vol. 40, # 3 p. 377 - 384
反应条件
1: 59.8 percent / dicyclohexylcarbodiimide / tetrahydrofuran / 20 °C 2: 55.8 percent / diphenylphosphoryl azide; triethylamine / 7 h / Heating 3: 90.4 percent / tetrabutylammonium bromide; K2CO3; NaOH / ethyl acetate / 0.17 h / 20 °C 4: 91.1 percent / trifluoroacetic acid / CH2Cl2 / 1 h / 20 °C View Scheme
参考文献
Synthetic Communications, , vol. 33, # 20 p. 3519 - 3526