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: With benzotriazol-1-ol; dicyclohexyl-carbodiimide 2: With hydrogen; platinum
参考文献
Cendrowska, Iwona; Bankowski, Krzysztof; Iskra-Jopa, Joanna
Acta Poloniae Pharmaceutica - Drug Research, 2003 , vol. 60, # 2 p. 141 - 144
反应条件
1: 1->3-(dimethylamino)propyl>-3-ethylcarbodiimide hydrochloride / dimethylformamide / 18 h / Ambient temperature 2: 4.6 g / NEt3 / dimethylformamide / Ambient temperature View Scheme
参考文献
Krapcho; Turk; Cushman; Powell; DeForrest; Spitzmiller; Karanewsky; Duggan; Rovnvak; Schwartz; Natarajan; Godfrey; Ryono; Neubeck; Atwa; Petrillo Jr.
Journal of Medicinal Chemistry, 1988 , vol. 31, # 6 p. 1148 - 1160
反应条件
pyridine; N,N'-disuccinimidyl-carbonate; triethylamine 1.) CH3CN, RT, 44 h, 2.) CH3CN, H2O, RT; Yield given. Multistep reaction;
参考文献
Smith, Elizabeth M.; Swiss, Gerald F.; Neustadt, Bernard R.; McNamara, Paul; Gold, Elijah H.; et al.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 7 p. 1600 - 1606
反应条件
1.1: HCl / CH2Cl2; dioxane / -5 - 0 °C 1.2: ClCOCOCl / dimethylformamide; CH2Cl2; dioxane / -5 - 0 °C 2.1: dimethylformamide; CH2Cl2; dioxane / 1 h / 20 °C 3.1: DBU / acetonitrile; CH2Cl2 / 8 h / 20 °C 3.2: 92 percent / ethyl acetate / 3 h / 20 °C View Scheme
参考文献
Palomo, Claudio; Palomo, Antonio L; Palomo, Francisco; Mielgo, Antonia
Organic letters, 2002 , vol. 4, # 23 p. 4005 - 4008
反应条件
O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; triethylamine in DMF (N,N-dimethyl-formamide); acetonitrile T=20°C; 0.5 h;
参考文献
LEK PHARMACEUTICALS D.D.
Patent: WO2004/101515 A1, 2004 ;
Location in patent: Page 9 ;
反应条件
1.1: HCl / CH2Cl2; dioxane / -5 - 0 °C 1.2: ClCOCOCl / dimethylformamide; CH2Cl2; dioxane / -5 - 0 °C 2.1: dimethylformamide; CH2Cl2; dioxane / 1 h / 20 °C 3.1: DBU / acetonitrile; CH2Cl2 / 8 h / 20 °C View Scheme
参考文献
Poechlauer, Peter; Hendel, Wolfram
Tetrahedron, 1998 , vol. 54, # 14 p. 3489 - 3494
反应条件
hydrogenchloride; phosphorus pentachloride in hexane
T=-5 - 10°C; 3 h;
参考文献
LUPIN LIMITED
Patent: WO2004/54980 A1, 2004 ;
Location in patent: Page 22-23;13;16 ;