(1S)-4,5-二甲氧基-1-(甲基氨基乙基)苯并环丁烷合成路线 （共 8 条）
反应条件
hydrogenchloride in ethanol; ethyl acetate T=15 - 20°C; 1 h; Industry scale;
参考文献
Lerestif, Jean-Michel; Blanco, Isaac Gonzalez; Lecouve, Jean-Pierre; Brigot, Daniel
Patent: US2005/261376 A1, 2005 ;
Location in patent: Page/Page column 3 ;
反应条件
1: in ethanol T=85°C; 1 h; AutoclaveInert atmosphere; 2: With trimethylamine-N-oxide; C34H51FeNO6SSi2; hydrogen in ethanol T=85°C; P=3750.38 Torr; 16 h; AutoclaveInert atmosphere; Reagent/catalyst;
参考文献
Les Laboratoires Servier; Renaud, Jean-Luc; Pannetier, Nicolas; Lecouve, Jean-Pierre; Vaysse-Ludot, Lucile; Moulin, Solenne
Patent: US8513410 B2, 2013 ;
Location in patent: Page/Page column 9; 10 ;
反应条件
1.1: potassium carbonate / 20 °C 2.1: potassium tert-butylate / dimethyl sulfoxide / 1 h / 20 °C 2.2: 20 °C View Scheme
参考文献
LES LABORATOIRES SERVIER
Patent: US2012/172589 A1, 2012 ;
反应条件
1: potassium carbonate / acetone / 18 h / |Reflux 2: acetic acid; hydrogen; palladium(II) oxide hydrate / 24 h / 20 °C / 3675.37 Torr View Scheme
参考文献
LES LABORATOIRES SERVIER; CARRANZA, Maria Del Pilar; GARCIA ARANDA, Maria Isabel; GONZALEZ, José Lorenzo; SANCHEZ, Frédéric
Patent: US2014/107334 A1, 2014 ;
反应条件
1: With potassium carbonate; sodium iodide in acetone T=20 - 65°C; 2: With triethylamine; acetyl chloride in toluene 3: With hydrogenchloride in water; toluene pH=2 - 3; Product distribution / selectivity;
参考文献
Alembic Pharmaceuticals Limited
Patent: EP2495237 A1, 2012 ;
Location in patent: Page/Page column 8 ;
反应条件
1.1: potassium carbonate / 20 °C 2.1: potassium tert-butylate / dimethyl sulfoxide / 1 h / 20 °C 2.2: 20 °C 3.1: hydrogenchloride / diethyl ether; acetonitrile View Scheme
参考文献
LES LABORATOIRES SERVIER
Patent: US2012/172589 A1, 2012 ;
反应条件
potassium carbonate in N,N-dimethyl-formamide
T=25 - 45°C; 12 h;
参考文献
KRKA, D. D., NOVO MESTO; BOSE, Prosenjit; SIRIPALLI, Udaya Bhaskara Rao; KANDADAI, Appan Srinivas
Patent: WO2010/72409 A1, 2010 ;
Location in patent: Page/Page column 20-21 ;
反应条件
1.1: potassium carbonate / 20 °C
2.1: potassium tert-butylate / dimethyl sulfoxide / 0.5 h / 20 °C
2.2: 20 °C
View Scheme
参考文献
LES LABORATOIRES SERVIER
Patent: US2012/208996 A1, 2012 ;
