N-[5-[N-[(3,4-二氢-2-甲基-4-氧-6-喹唑啉基)甲基]-N-甲基氨基]-2-噻吩甲酰]-L-谷氨酸二乙酯合成路线 (共 13 条)
反应条件
2,6-dimethylpyridine in N,N-dimethyl-formamide T=55 - 60°C;
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
1: 91.1 percent / trifluoroacetic acid / CH2Cl2 / 1 h / 20 °C 2: 74.2 percent / 2,6-lutidine / dimethylformamide / 55 - 60 °C View Scheme
参考文献
Synthetic Communications, , vol. 33, # 20 p. 3519 - 3526
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 4: 22 percent / 2,6-lutidine / various solvent(s) / 18 h / 80 °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 4: 22 percent / 2,6-lutidine / various solvent(s) / 18 h / 80 °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 5: 22 percent / 2,6-lutidine / various solvent(s) / 18 h / 80 °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 4: 22 percent / 2,6-lutidine / various solvent(s) / 18 h / 80 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 5 p. 1594 - 1605
反应条件
1: 48 percent / 2,6-lutidine / dimethylformamide; toluene / 24 h / 70 °C 2: 22 percent / 2,6-lutidine / various solvent(s) / 18 h / 80 °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 3: 22 percent / 2,6-lutidine / various solvent(s) / 18 h / 80 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 5 p. 1594 - 1605
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 5: 74.2 percent / 2,6-lutidine / dimethylformamide / 55 - 60 °C View Scheme
参考文献
Synthetic Communications, , vol. 33, # 20 p. 3519 - 3526
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 5: 74.2 percent / 2,6-lutidine / dimethylformamide / 55 - 60 °C View Scheme
参考文献
Synthetic Communications, , vol. 33, # 20 p. 3519 - 3526