4-[4-[(5S)-5-(氨基甲基)-2-氧代-3-恶唑烷基]苯基]-3-吗啉酮盐酸盐合成路线 （共 15 条）
反应条件
1: 4-[4-{(R)-3-amino-2-hydroxypropylamino}phenyl]morpholin-3-one hydrochloride With potassium carbonate in isobutyl methylketone T=4°C; Inert atmosphereReflux; 2: 1,1'-carbonyldiimidazole in isobutyl methylketone T=20°C; 15 h; 3: With hydrogenchloride in water; isobutyl methylketone
参考文献
SANDOZ AG; STURM, Hubert; KNEPPER, Kerstin
Patent: WO2012/140061 A1, 2012 ;
Location in patent: Page/Page column 36 ;
反应条件
hydrogenchloride; water in ethanol T=50°C; 2 h; Inert atmosphere;
参考文献
SANDOZ AG; STURM, Hubert; KNEPPER, Kerstin
Patent: WO2012/140061 A1, 2012 ;
Location in patent: Page/Page column 30 ;
反应条件
hydrogenchloride in methanol T=20°C; 1 h;
参考文献
SYMED LABS LIMITED; MOHAN RAO, Dodda; KRISHNA REDDY, Pingili; VENKAT REDDY, Buthukuri
Patent: WO2013/46211 A1, 2013 ;
Location in patent: Page/Page column 63 ;
反应条件
1.1: ethanol / 9 h / 80 °C 2.1: tetrahydrofuran / 4 h / |Reflux 3.1: methylamine / ethanol; water / 2 h / 65 °C 3.2: 65 °C / pH 2.7 View Scheme
反应条件
1.1: tetrahydrofuran / 4 h / |Reflux 2.1: methylamine / ethanol; water / 2 h / 65 °C 2.2: 65 °C / pH 2.7 View Scheme
反应条件
1: lithium tert-butylate / N,N-dimethyl-formamide; methanol / 18 h / 0 - 25 °C 2: hydrogenchloride / methanol / 1 h / 20 °C View Scheme
反应条件
1.1: ammonia / water / 4 h / 20 °C 2.1: potassium carbonate / isobutyl methylketone / 4 °C / Inert atmosphere; Reflux 2.2: 15 h / 20 °C View Scheme
反应条件
1: sodium iodide / sulfolane / 20 h / 110 °C 2: sulfolane / 72 h / 50 °C / Inert atmosphere 3: hydrogenchloride; water / ethanol / 2 h / 50 °C / Inert atmosphere View Scheme
反应条件
1: sulfolane / 72 h / 50 °C / Inert atmosphere 2: hydrogenchloride; water / ethanol / 2 h / 50 °C / Inert atmosphere View Scheme
反应条件
1: dichloromethane / 44 h / 20 °C 2: hydrogenchloride / methanol / 1 h / 20 °C View Scheme
