(R)-4-[4-[(3-氯-2-羟基丙基)氨基]苯基]吗啉-3-酮合成路线 (共 5 条)
反应条件
1.1: N,N-dimethyl-formamide / 3 h / 20 - 100 °C 2.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 4.05 h / 20 °C 3.1: oxalyl dichloride / dichloromethane; N,N-dimethyl-formamide / 3.08 h / 0 °C / Cooling with ice 3.2: 0.08 h / 0 °C 4.1: potassium carbonate; methylamine / isopropyl alcohol; water / 15 h / 60 °C View Scheme
参考文献
SANDOZ AG; STURM, Hubert; KNEPPER, Kerstin
Patent: WO2012/140061 A1, 2012 ;
反应条件
in N,N-dimethyl-formamide T=20 - 100°C; 3 h;
参考文献
APOTEX PHARMACHEM INC.; BODHURI, Prabhudas; WEERATUNGA, Gamini
Patent: WO2012/51692 A1, 2012 ;
Location in patent: Page/Page column 42-43 ;
反应条件
in N,N-dimethyl-formamide 5 h; Reflux;
参考文献
SYMED LABS LIMITED; MOHAN RAO, dodda; KRISHNA REDDY, pingili; ANNA REDDY, ambati; VENKAT REDDY, buthukuri
Patent: WO2012/32533 A2, 2012 ;
Location in patent: Page/Page column 16 ;
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
参考文献
SANDOZ AG; STURM, Hubert; KNEPPER, Kerstin
Patent: WO2012/140061 A1, 2012 ;
反应条件
Multi-step reaction with 2 steps 1: acetonitrile / 3 h / 20 °C / Inert atmosphere2: sodium iodide / sulfolane / 20 h / 110 °C
参考文献
SANDOZ AG; STURM, Hubert; KNEPPER, Kerstin Patent: WO2012/140061 A1, 2012 ;