N-[1-(S)-乙氧羰基-3-苄丙基]-L-丙氨酸-N-羰甲醛合成路线 (共 14 条)
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
triethylamine in dichloromethane T=20°C;
参考文献
INSTYTUT FARMACEUTYCZNY
Patent: WO2005/108366 A1, 2005 ;
Location in patent: Page/Page column 12 ;
反应条件
1: 2,3,3a,4,5,6-hexahydrocyclopenta[b]pyrrole-2-carboxylic acid; (S,S,S)-2-azabicyclolt;3.3.0gt;octane-3-carboxylic acid hydrochloride With sodium hydroxide; hydrogenation catalyst in water T=20 - 25°C; pH=10 - 11; 2: N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride in water T=20 - 25°C; pH=10 - 11; 3 - 4 h; 3: With hydrogenchloride in water T=15 - 20°C; pH=4.4 - 5.2; 2.5 - 2.75 h; Product distribution / selectivity;
参考文献
sanofi-aventis Deutschland GmbH
Patent: US2009/17509 A1, 2009 ;
Location in patent: Page/Page column 7 ;
反应条件
1: in water; ethyl acetate T=19 - 20°C; pH=10 - 11; 5 h; 2: T=30°C; pH=4.3 - 4.7; 0.166667 h;
参考文献
US6335453 B1, ;
Example 1 ;
反应条件
1: N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride With 1,1'-carbonyldiimidazole in tetrahydrofuran T=20°C; 1 h; 2: sodium (indan-2-yl)glycinate in tetrahydrofuran T=20°C; 3 h; 3: With hydrogenchloride in water pH=2 - 3; Product distribution / selectivity;
参考文献
DIPHARMA FRANCIS s.r.l.
Patent: US2008/15383 A1, 2008 ;
Location in patent: Page/Page column 3 ;
反应条件
1: (2S,3aR,7aS)-octahydroindolecarboxylic acid With triethylamine in dichloromethane T=20°C; 0.5 h; 2: N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride in dichloromethane T=20°C; 3 h; 3: With hydrogenchloride in dichloromethane; water T=15°C; pH=4.2; Product distribution / selectivity;
参考文献
CIPLA LIMITED; CURTIS, Philip, Anthony
Patent: WO2007/3947 A2, 2007 ;
Location in patent: Page/Page column 9; 12-14 ;
反应条件
1: in dichloromethane T=0 - 5°C; 2 h; 2: With acetic acid in water Product distribution / selectivity;
参考文献
Glenmark Pharmaceuticals Limited
Patent: US2006/79698 A1, 2006 ;
Location in patent: Page/Page column 6 ;
反应条件
triethylamine in water; acetone T=0 - 25°C; pH=9.0 - 10.6; 2 h; Product distribution / selectivity;
参考文献
AZAD PHARMACEUTICALS INGREDIENTS AG
Patent: WO2005/51909 A1, 2005 ;
Location in patent: Page/Page column 6; 18-19; 20 ;