N-(4-氨基苯(甲)酰)-L-谷氨酸二乙酯合成路线 （共 22 条）
反应条件
1: 94 percent / sodium cyanoborohydride, bromocresol green, acetic acid / ethanol / 48 h / Ambient temperature 2: 91 percent / sodium cyanoborohydride, bromocresol green, aq. acetic acid / acetonitrile / 1 h / Ambient temperature 3: 80 percent / hydrogen, HCl / palladium on carbon / ethanol / 3 h / 2482.3 Torr View Scheme
参考文献
Yang; Slusher; Broom; Ueda; Cheng
Journal of Medicinal Chemistry, 1988 , vol. 31, # 11 p. 2126 - 2132
反应条件
in dichloromethane; ethyl acetate; N,N-dimethyl-formamide
参考文献
National Research Development Corporation
Patent: US5236927 A1, 1993 ;
反应条件
1: N,N-dimethyl acetamide / 48 h / 20 °C
2: sodium hydroxide / tetrahydrofuran / 20 °C
View Scheme
参考文献
Zhang, Zhili; Tian, Chao; Zhou, Shouxin; Wang, Wei; Guo, Ying; Xia, Jie; Liu, Zhenming; Wang, Biao; Wang, Xiaowei; Golding, Bernard T.; Griff, Roger J.; Du, Yansheng; Liu, Junyi
European Journal of Medicinal Chemistry, 2012 , vol. 58, p. 228 - 236
反应条件
hydrogen; acetic acid; nickel
T=20 - 23°C; P=724.007 - 775.7 Torr; 14 h;
参考文献
Piper, J. R.; McCaleb, G. S.; Montgomery, J. A.; Kisliuk, R. L.; Gaumont, Y.; Sirotnak, F. M.
Journal of Medicinal Chemistry, 1986 , vol. 29, # 6 p. 1080 - 1087
反应条件
hydrogen; acetic acid; nickel
T=25°C; 17 h;
参考文献
Temple, Carroll; Elliott, Robert D.; Montgomery, John A.
Journal of Organic Chemistry, 1982 , vol. 47, # 5 p. 761 - 764
反应条件
in AcOH--H2 O; ethanol
参考文献
Southern Research Institute; Sloan-Kettering Institute for Cancer Research
Patent: US4725687 A1, 1988 ;
反应条件
in N,N-dimethyl acetamide
72 h; Ambient temperature; Yield given;
参考文献
Su, Tsann-Long; Huang, Jai-Tung; Burchenal, Joseph H.; Watanabe, Kyoichi A.; Fox, Jack J.
Journal of Medicinal Chemistry, 1986 , vol. 29, # 5 p. 709 - 715
反应条件
1: 32 percent / 70percent CH3COOH, H2 / Raney Ni / 17 h / 25 °C
2: 87 percent / 1 N NaOH / dimethylsulfoxide / 6 h
3: 94 percent / NaBH3CN / H2O / 23 h / pH 6.4
View Scheme
参考文献
Temple, Carroll; Elliott, Robert D.; Montgomery, John A.
Journal of Organic Chemistry, 1982 , vol. 47, # 5 p. 761 - 764
反应条件
1: 32 percent / 70percent CH3COOH, H2 / Raney Ni / 17 h / 25 °C
2: 87 percent / 1 N NaOH / dimethylsulfoxide / 6 h
3: 94 percent / NaBH3CN / H2O / 23 h / pH 6.4
4: 64 percent / 1 N NaOH / 4.25 h / Heating
View Scheme
参考文献
Temple, Carroll; Elliott, Robert D.; Montgomery, John A.
Journal of Organic Chemistry, 1982 , vol. 47, # 5 p. 761 - 764
反应条件
1: NaHCO3 / toluene; ethanol / 16 h / Heating
2: 52 percent / N,N-dimethyl-acetamide / 1.) 25 deg C, 18 h, 2.) 60 deg C, 6 h, 3.) 80 deg C, 1 h
3: 81 percent / 1N aq. NaOH / methanol / 1.) 25 deg C, 18 h, 2.) reflux, 1 h
View Scheme
参考文献
Piper, J. R.; McCaleb, G. S.; Montgomery, J. A.; Kisliuk, R. L.; Gaumont, Y.; Sirotnak, F. M.
Journal of Medicinal Chemistry, 1982 , vol. 25, # 7 p. 877 - 880
