Boc-beta-丙氨酸合成路线 （共 48 条）
参考文献
Weitman, Michal; Lerman, Keti; Nudelman, Abraham; Major, Dan Thomas; Hizi, Amnon; Herschhorn, Alon
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 2 p. 447 - 467
反应条件
in dichloromethane T=0°C; 2 h;
参考文献
Kolb, Hartmuth C.; Kanamarlapudi, Ramanaiah C.; Richardson, Paul F.
Patent: US2004/19215 A1, 2004 ;
Location in patent: Page 5 ;
反应条件
1: NMM / tetrahydrofuran / 0.33 h / -20 °C 2: NaN3 / tetrahydrofuran; H2O / 0.08 h / -5 °C 3: toluene / 0.17 h / 65 °C 4: 3.3 g / pyridine / toluene / 0.08 h / 65 °C View Scheme
参考文献
Pendem, Nagendar; Douat, Celine; Claudon, Paul; Laguerre, Michel; Castano, Sabine; Desbat, Bernard; Cavagnat, Dominique; Ennifar, Eric; Kauffmann, Brice; Guichard, Gilles
Journal of the American Chemical Society, 2013 , vol. 135, # 12 p. 4884 - 4892
反应条件
1: 4-(N,N-dimethlyamino)pyridine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 3.5 h / 0 - 20 °C / Inert atmosphere 2: ethyl acetate / 3 h / Inert atmosphere; Reflux View Scheme
参考文献
NOVARTIS AG; BOCK, Mark G.; GAUL, Christoph; GUMMADI, Venkateshwar Rao; MOEBITZ, Henrik; SENGUPTA, Saumitra
Patent: WO2012/35078 A1, 2012 ;
WO 2012/035078 A1
反应条件
4-(N,N-dimethlyamino)pyridine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride in dichloromethane T=0 - 25°C; 5 h; Inert atmosphere;
参考文献
Xin, Dongyue; Perez, Lisa M.; Ioerger, Thomas R.; Burgess, Kevin
Angewandte Chemie - International Edition, 2014 , vol. 53, # 14 p. 3594 - 3598
Angew. Chem., 2014 , vol. 126, # 14 p. 3668 - 3672,5
反应条件
1: 70 percent / EEDQ, NH4HCO3 / CHCl3 / 20 °C 2: 70 percent / Lawesson's reagent / tetrahydrofuran / 24 h / 20 °C View Scheme
参考文献
Josse, Olivier; Labar, Daniel; Marchand-Brynaert, Jacqueline
Synthesis, 1999 , # 3 p. 404 - 406
反应条件
1: 1.) Et3N, ethyl carbonochloridate, 2.) 20percent aq. NH3 / 1.) THF, -10 deg C, 20 min., 2.) -10 deg C to room temp., overnight 2: 93 percent / Et3N, trifluoroacetic anhydride / tetrahydrofuran / 1 h / 0 deg C to room temp., 3: 59 percent / NH3, H2 / Raney Ni / ethanol / 8 h / 50 °C / 15514.4 Torr View Scheme
参考文献
Houssin, Raymond; Bernier, Jean-Luc; Henichart, Jean-Pierre
Synthesis, 1988 , # 3 p. 259 - 261
反应条件
1: N-tert-butoxycarbonyl-β-alanine With 1,1'-carbonyldiimidazole in tetrahydrofuran T=0 - 20°C; 1 h; 2: EtOCOC(NH2)NOH With pyridine in tetrahydrofuran 2 h; Heating / reflux;
参考文献
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Patent: WO2006/62224 A1, 2006 ;
Location in patent: Page/Page column 64 ;
反应条件
1.1: N-methylmorpholine; isobutylchloroformate / CH2Cl2 / 0.25 h / -15 °C 1.2: 100 percent / CH2Cl2 / 16 h / -15 - 20 °C 2.1: 64 percent / LiAlH4 / tetrahydrofuran / 0.33 h / 20 °C View Scheme
参考文献
Bitan, Gal; Muller, Dan; Kasher, Ron; Gluhov, Evgenia V.; Gilon, Chaim
Journal of the Chemical Society - Perkin Transactions 1, 1997 , # 10 p. 1501 - 1510
反应条件
1: 1.) Et3N, ethyl carbonochloridate, 2.) 20percent aq. NH3 / 1.) THF, -10 deg C, 20 min., 2.) -10 deg C to room temp., overnight 2: 93 percent / Et3N, trifluoroacetic anhydride / tetrahydrofuran / 1 h / 0 deg C to room temp., View Scheme
参考文献
Houssin, Raymond; Bernier, Jean-Luc; Henichart, Jean-Pierre
Synthesis, 1988 , # 3 p. 259 - 261
