(3R,4S)-1-(4-氟苯基)-3-[3-(4-氟苯基)-3-氧代丙基]-4-(4-羟基苯基)氮杂环丁烷-2-酮合成路线 (共 23 条)
反应条件
hydrogen; palladium on activated charcoal in ethanol P=3102.9 Torr; 12 h;
参考文献
Journal of Medicinal Chemistry, , vol. 41, # 6 p. 973 - 980
反应条件
hydrogen; palladium on activated charcoal in methanol; ethyl acetate Hydrogenation; P=1551.44 Torr; 3 h;
参考文献
Wu; Wong; Chen; Ding
Journal of Organic Chemistry, 1999 , vol. 64, # 10 p. 3714 - 3718
反应条件
1: With water; acetic acid in tetrahydrofuran T=60°C; 5 h; 2: With water; sodium hydrogencarbonate in toluene Product distribution / selectivity;
参考文献
ZENTIVA, A.S.
Patent: WO2008/106900 A1, 2008 ;
Location in patent: Page/Page column 12 ;
反应条件
formic acid T=20 - 25°C; 1 h; Product distribution / selectivity;
参考文献
WO2007/120824 A2, ;
Page/Page column 75 ;
反应条件
1: (nBu)3N / heptane; toluene / 80 - 90 °C 2: LiOH*H2O / methanol / 2 h 3: oxalyl chloride / CH2Cl2 / 16 h / 22 °C 4: (Ph3P)4Pd / tetrahydrofuran / 1 h / 10 °C 5: H2 / 10percent Pd/C / ethanol / 12 h / 3102.9 Torr View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 41, # 6 p. 973 - 980
反应条件
1: oxalyl chloride / CH2Cl2 / 16 h / 22 °C 2: (Ph3P)4Pd / tetrahydrofuran / 1 h / 10 °C 3: H2 / 10percent Pd/C / ethanol / 12 h / 3102.9 Torr View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 41, # 6 p. 973 - 980
反应条件
1: (Ph3P)4Pd / tetrahydrofuran / 1 h / 10 °C 2: H2 / 10percent Pd/C / ethanol / 12 h / 3102.9 Torr View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 41, # 6 p. 973 - 980
反应条件
1: LiOH*H2O / methanol / 2 h 2: oxalyl chloride / CH2Cl2 / 16 h / 22 °C 3: (Ph3P)4Pd / tetrahydrofuran / 1 h / 10 °C 4: H2 / 10percent Pd/C / ethanol / 12 h / 3102.9 Torr View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 41, # 6 p. 973 - 980
反应条件
1: 64 percent / LDA; DMPU; LiCl / dimethylformamide; tetrahydrofuran / 18 h / -30 - -25 °C 2: 90 percent / NaIO4 / acetonitrile; H2O / 2 h / 20 °C 3: BF3 etherate / toluene / 0.08 h / -30 °C 4: 99 g / p-toluenesulfonic acid monohydrate; molecular sieves / toluene / 4 h / 40 - 50 °C 5: 90 percent / hydrogen / 10 percent Pd/C / methanol; ethyl acetate / 3 h / 1551.44 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 64, # 10 p. 3714 - 3718
反应条件
1: BF3 etherate / toluene / 0.08 h / -30 °C 2: 99 g / p-toluenesulfonic acid monohydrate; molecular sieves / toluene / 4 h / 40 - 50 °C 3: 90 percent / hydrogen / 10 percent Pd/C / methanol; ethyl acetate / 3 h / 1551.44 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 64, # 10 p. 3714 - 3718