N-[1-(S)-乙氧羰基-3-苯丙基]-L-丙氨酸合成路线 （共 47 条）
反应条件
1.1: triphenylphosphine / CH2Cl2 / 0.75 h 1.2: 45 percent / CH2Cl2 / 2.5 h / 25 - 30 °C 2.1: triethylamine / CH2Cl2 / 4 h / -15 - -10 °C 3.1: hydrogen / Pd/C View Scheme
参考文献
Singh, Girij Pal; Godbole, Himanshu M.; Nehate, Sagar P.; Mahajan, Pravin R.
Synthetic Communications, 2005 , vol. 35, # 2 p. 243 - 248
反应条件
1: DCC / tetrahydrofuran / Ambient temperature 2: 1) tBuOK / 1) THF, -50 deg C, 20 min, 2) THF, -30 deg C, 20 min 3: ethyl acetate; diisopropyl ether / 3 h / Ambient temperature 4: 1) K2CO3, 2) 15percent HCl/dioxane / 1) H2O, 2) rt, overnight View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 32, # 2 p. 289 - 297
反应条件
1.1: triphenylphosphine / CH2Cl2 / 0.75 h 1.2: 45 percent / CH2Cl2 / 2.5 h / 25 - 30 °C 2.1: triethylamine / CH2Cl2 / 4 h / -15 - -10 °C 3.1: hydrogen / Pd/C View Scheme
参考文献
Singh, Girij Pal; Godbole, Himanshu M.; Nehate, Sagar P.; Mahajan, Pravin R.
Synthetic Communications, 2005 , vol. 35, # 2 p. 243 - 248
反应条件
in dichloromethane T=0 - 5°C; 1 h;
参考文献
US2006/79698 A1, ;
Page/Page column 6 ;
反应条件
1: in dichloromethane T=20 - 30°C; 14 - 16 h; Heating / reflux; 2: With sodium hydrogencarbonate in water; acetone T=0 - 20°C; 0.5 - 1.5 h; Product distribution / selectivity;
参考文献
WO2005/51909 A1, ;
Page/Page column 6; 18; 20 ;
反应条件
in tetrahydrofuran; toluene 2.5 h; Heating;
参考文献
European Journal of Medicinal Chemistry, , vol. 20, # 6 p. 563 - 570
反应条件
1.1: triphenylphosphine / CH2Cl2 / 0.75 h 1.2: 45 percent / CH2Cl2 / 2.5 h / 25 - 30 °C 2.1: triethylamine / CH2Cl2 / 4 h / -15 - -10 °C View Scheme
参考文献
Singh, Girij Pal; Godbole, Himanshu M.; Nehate, Sagar P.; Mahajan, Pravin R.
Synthetic Communications, 2005 , vol. 35, # 2 p. 243 - 248
反应条件
1: With benzotriazol-1-ol; dicyclohexyl-carbodiimide in dichloromethane T=20 - 25°C; 3 h; 2: With hydrogen; palladium 10 on activated carbon in isopropyl alcohol T=25 - 35°C; P=1471.14 - 2206.72 Torr; 3: With diethyl ether 0.0833333 - 0.166667 h;
参考文献
DR. REDDY'S LABORATORIES LTD.; DR. REDDY'S LABORATORIES, INC.
Patent: WO2006/14916 A2, 2006 ;
Location in patent: Page/Page column 5 ;
反应条件
1: With benzotriazol-1-ol; dicyclohexyl-carbodiimide in dichloromethane T=20 - 25°C; 3 h; 2: With hydrogen; palladium 10 on activated carbon in isopropyl alcohol T=25 - 35°C; P=1471.14 - 2206.72 Torr;
参考文献
DR. REDDY'S LABORATORIES LTD.; DR. REDDY'S LABORATORIES, INC.
Patent: WO2006/14916 A2, 2006 ;
Location in patent: Page/Page column 5 ;
反应条件
1: phenylmethyl-(2S,3aR,7aS)-octahydroindole-2-carboxylate hydrochloride With sodium hydroxide in dichloromethane; water 1 h; 2: (2S)-2-[N-((1S)-1-ethoxycarbonyl-3-phenylpropyl)amino]propionic acid With benzotriazol-1-ol; triethylamine; dicyclohexyl-carbodiimide in dichloromethane T=20°C; 20.25 h; 3: With hydrogen; palladium 10 on activated carbon in ethanol P=1500.15 Torr; Product distribution / selectivity;
参考文献
Sochinaz SA
Patent: EP1724260 A1, 2006 ;
Location in patent: Page/Page column 14-15 ;
