(2R,3S)-2-[(1R)-1-[3,5-双(三氟甲基)苯基)乙氧基]-3-(4-氟苯基)吗啉合成路线 (共 20 条)
反应条件
1.1: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 2.1: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C 3.1: tetrahydrofuran / 20 - 30 °C 3.2: H2 / 10 percent Pd/C / methanol; tetrahydrofuran View Scheme
参考文献
Journal of the American Chemical Society, , vol. 125, # 8 p. 2129 - 2135
反应条件
1.1: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 2.1: tetrahydrofuran / 20 - 30 °C 2.2: H2 / 10 percent Pd/C / methanol; tetrahydrofuran View Scheme
参考文献
Journal of the American Chemical Society, , vol. 125, # 8 p. 2129 - 2135
反应条件
1.1: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C 2.1: tetrahydrofuran / 20 - 30 °C 2.2: H2 / 10 percent Pd/C / methanol; tetrahydrofuran View Scheme
参考文献
Journal of the American Chemical Society, , vol. 125, # 8 p. 2129 - 2135
反应条件
1: K2CO3 / toluene / 5 h / 20 °C 2: 14.3 g / BF3*Et2O / tetrahydrofuran / 1 h / -20 °C 3: TsOH*H2O; hydrogen / 5percent Pd/C / ethanol; toluene / 3 h / 30 °C / 2068.65 Torr 4: NCS; K2CO3 / dimethylformamide / 0.5 h / 0 °C 5: DBU / dimethylformamide / 3 h / 0 - 20 °C 6: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 67, # 19 p. 6743 - 6747
反应条件
1: 14.3 g / BF3*Et2O / tetrahydrofuran / 1 h / -20 °C 2: TsOH*H2O; hydrogen / 5percent Pd/C / ethanol; toluene / 3 h / 30 °C / 2068.65 Torr 3: NCS; K2CO3 / dimethylformamide / 0.5 h / 0 °C 4: DBU / dimethylformamide / 3 h / 0 - 20 °C 5: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 67, # 19 p. 6743 - 6747
反应条件
1: NCS; K2CO3 / dimethylformamide / 0.5 h / 0 °C 2: DBU / dimethylformamide / 3 h / 0 - 20 °C 3: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 67, # 19 p. 6743 - 6747
反应条件
1: TsOH*H2O; hydrogen / 5percent Pd/C / ethanol; toluene / 3 h / 30 °C / 2068.65 Torr 2: NCS; K2CO3 / dimethylformamide / 0.5 h / 0 °C 3: DBU / dimethylformamide / 3 h / 0 - 20 °C 4: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 67, # 19 p. 6743 - 6747
反应条件
sodium tetrahydroborate in methanol T=0 - 5°C; Large scale reaction;
参考文献
Gangula, Srinivas; Elati, Chandrashekhar R.; Mudunuru, Satish Varma; Nardela, Anitha; Dongamanti, Ashok; Bhattacharya, Apurba; Bandichhor, Rakeshwar
Synthetic Communications, 2010 , vol. 40, # 15 p. 2254 - 2268
反应条件
potassium carbonate in N,N-dimethyl-formamide T=20°C; 0.5 h;
参考文献
Sandoz AG
Patent: WO2009/106486 A1, 2009 ;
Location in patent: Page/Page column 18 ;
反应条件
1: With N-ethyl-N,N-diisopropylamine in acetonitrile T=20°C; 3 h; 2: in acetonitrile T=110°C; P=1125.11 Torr; 55 h; Product distribution / selectivity;
参考文献
Sandoz AG
Patent: WO2009/106486 A1, 2009 ;
Location in patent: Page/Page column 18-19 ;