(3R,4S)-1-(4-氟苯基)-3-[(3S)-3-(4-氟苯基)-3-羟基丙基]-4-[4-(苯甲氧基)苯基]-2-氮杂环丁酮合成路线 (共 37 条)
反应条件
1: potassium iodide / acetonitrile; water / 0.58 h / 20 °C 2: Burgess Reagent / toluene / 18 h / 90 °C 3: platinum(IV) oxide; hydrogen / toluene / 20 °C / 750.08 Torr 4: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1: platinum(IV) oxide; hydrogen / toluene / 20 °C / 750.08 Torr 2: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 1.2: 0.25 h / 20 °C 2.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 3.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 4.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
5 Pd(II)/C(eggshell); hydrogen in ethanol T=20°C; P=3102.97 Torr;
参考文献
Sniezek, Marcin; Stecko, Sebastian; Panfil, Irma; Furman, Bartlomiej; Chmielewski, Marek
Journal of Organic Chemistry, 2013 , vol. 78, # 14 p. 7048 - 7057
反应条件
formic acid; ammonium formate; 5-palladium/activated carbon in methanol T=20°C; Inert atmosphere; Product distribution / selectivity;
参考文献
Lek Pharmaceuticals D.D.
Patent: EP2128133 A1, 2009 ;
Location in patent: Page/Page column 5-6 ;
反应条件
1: H2 / 10percent Pd/C / ethanol / 16 h / 3102.9 Torr 2: 0.260 g / pyridine / CH2Cl2 / 1 h / 22 °C View Scheme
参考文献
Rosenblum, Stuart B.; Huynh, Tram; Afonso, Adriano; Davis Jr., Harry R.; Yumibe, Nathan; Clader, John W.; Burnett, Duane A.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 6 p. 973 - 980
反应条件
formic acid; ammonium formate; 5-palladium/activated carbon in methanol T=20°C; Inert atmosphere; Product distribution / selectivity;
参考文献
Lek Pharmaceuticals D.D.
Patent: EP2128133 A1, 2009 ;
Location in patent: Page/Page column 5-6 ;