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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
1313613-18-1
合成路线
（共 8 条）
1313613-18-1
+
1325210-61-4
→
反应条件
366789-02-8
利伐沙班
反应条件
1: 5-chloro-thiophene-2-carboxylic acid (S)-2-hydroxy-3-tosyloxy-propyl-amide With pyridine; acetic anhydride T=0°C; 1 h; 2: With hydrogenchloride in tert-butyl methyl ether; water pH=2; 3: [4-(3-oxo-morpholin-4-yl)phenyl]carbamic acid benzyl ester With lithium tert-butylate in methanol; acetonitrile T=0°C; 17 h;
参考文献
SANDOZ AG; STURM, Hubert; DE SOUZA, Dominic; KNEPPER, Kerstin; ALBERT, Martin
Patent: WO2011/98501 A1, 2011 ;
Location in patent: Page/Page column 30; 31 ;
1313613-18-1
+
1384257-81-1
→
反应条件
366789-02-8
利伐沙班
反应条件
lithium tert-butylate in tetrahydrofuran; N,N-dimethyl-formamide T=20°C; 44 h; Cooling with ice;
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 50; 51 ;
1313613-18-1
→
反应条件
366789-02-8
利伐沙班
反应条件
lithium tert-butylate in tetrahydrofuran; methanol; N,N-dimethyl-formamide T=5 - 21°C; 21 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 50 ;
1313613-18-1
→
反应条件
366789-02-8
利伐沙班
反应条件
1.1: lithium tert-butylate / tetrahydrofuran / 24 h / 20 °C 2.1: triethylamine / dichloromethane / 4 h / 20 °C 3.1: isopropyl alcohol / 12 h / 120 °C 4.1: triethylamine / dichloromethane / 24 h / 20 °C 5.1: hydrogenchloride / ethyl acetate / 2 h / 55 °C 5.2: pH 9 View Scheme
参考文献
ENANTIA, S.L.; RAFECAS JANE, Llorenc; COMELY, Alexander Christian; FERRALI, Alessandro; AMELA CORTES, Celia; PASTO AGUILA, Mireia
Patent: WO2011/80341 A1, 2011 ;
1313613-18-1
+
1429333-89-0
→
反应条件
366789-02-8
利伐沙班
反应条件
1: lithium tert-butylate / N,N-dimethyl-formamide; tetrahydrofuran / 44 h / 20 °C / |Cooling with ice 2: N-methyl-acetamide; N-bromosuccinmide / chloroform / 18 h / 30 °C / |Reflux View Scheme
参考文献
SYMED LABS LIMITED; MOHAN RAO, Dodda; KRISHNA REDDY, Pingili; VENKAT REDDY, Buthukuri
Patent: WO2013/46211 A1, 2013 ;
1313613-18-1
+
1429333-88-9
→
反应条件
366789-02-8
利伐沙班
反应条件
1: lithium tert-butylate / N,N-dimethyl-formamide; methanol; tetrahydrofuran / 21 h / 5 - 24 °C 2: N-methyl-acetamide; N-bromosuccinmide / chloroform / 18 h / 30 °C / |Reflux View Scheme
参考文献
SYMED LABS LIMITED; MOHAN RAO, Dodda; KRISHNA REDDY, Pingili; VENKAT REDDY, Buthukuri
Patent: WO2013/46211 A1, 2013 ;
1313613-18-1
+
1429333-92-5
→
反应条件
366789-02-8
利伐沙班
反应条件
1: lithium tert-butylate / N,N-dimethyl-formamide; tetrahydrofuran / 44 h / 20 °C / |Cooling with ice 2: N-methyl-acetamide; N-bromosuccinmide / chloroform / 18 h / 30 °C / |Reflux View Scheme
参考文献
SYMED LABS LIMITED; MOHAN RAO, Dodda; KRISHNA REDDY, Pingili; VENKAT REDDY, Buthukuri
Patent: WO2013/46211 A1, 2013 ;
1313613-18-1
→
反应条件
898543-06-1
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
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
参考文献
SYMED LABS LIMITED; MOHAN RAO, Dodda; KRISHNA REDDY, Pingili; VENKAT REDDY, Buthukuri
Patent: WO2013/46211 A1, 2013 ;
