[4-(4-氨基苯氧基)(2-吡啶基)]-N-(甲基-d3)甲酰胺合成路线 (共 9 条)
反应条件
1: 4-amino-phenol With potassium tert-butylate in N,N-dimethyl-formamide T=20°C; 2 h; 2: 4-chloro-N-(methyl-d3)picolinamide With potassium carbonate in N,N-dimethyl-formamide T=80°C;
参考文献
SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD; Feng, Weidong; Gao, Xiaoyong; Dai, Xiaojun
Patent: US2013/60043 A1, 2013 ;
Location in patent: Paragraph 0129; 0130 ;
反应条件
1.1: thionyl chloride; N,N-dimethyl-formamide / 16.33 h / 40 - 72 °C / |Reflux 2.1: tetrahydrofuran / 5 h / 5 °C 3.1: potassium tert-butylate / N,N-dimethyl-formamide / 2 h / 20 °C 3.2: 80 °C View Scheme
参考文献
SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD; Feng, Weidong; Gao, Xiaoyong; Dai, Xiaojun
Patent: US2013/60043 A1, 2013 ;
反应条件
1.1: tetrahydrofuran / 5 h / 5 °C 2.1: potassium tert-butylate / N,N-dimethyl-formamide / 2 h / 20 °C 2.2: 80 °C View Scheme
参考文献
SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD; Feng, Weidong; Gao, Xiaoyong; Dai, Xiaojun
Patent: US2013/60043 A1, 2013 ;
反应条件
1.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 16 h / 20 °C 2.1: potassium tert-butylate / N,N-dimethyl-formamide / 2 h / 20 °C 2.2: 20 - 80 °C View Scheme
参考文献
SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.; Feng, Weidong; Gao, Xiaoyong; Dai, Xiaojun
Patent: US2013/35492 A1, 2013 ;
反应条件
1.1: thionyl chloride / N,N-dimethyl-formamide / 16.33 h / 40 - 72 °C 2.1: tetrahydrofuran / 5 h / 5 °C 3.1: potassium tert-butylate / N,N-dimethyl-formamide / 2 h / 20 °C 3.2: 80 °C View Scheme
参考文献
SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.; Xing, Lidong; Sheng, Zelin; Wu, Guozhang; Lu, Huiping
Patent: US2013/12548 A1, 2013 ;
反应条件
1.1: potassium carbonate / tetrahydrofuran / 20 h / 20 °C 2.1: potassium tert-butylate / N,N-dimethyl-formamide / 2 h / 20 °C 2.2: 20 - 80 °C View Scheme
参考文献
SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD; Feng, Weidong; Gao, Xiaoyong; Dai, Xiaojun
Patent: US2013/60043 A1, 2013 ;
反应条件
1: 4-Chloro-3-(trifluoromethyl)benzenamine; 1,1'-carbonyldiimidazole in dichloromethane T=20°C; 16 h; 2: 4-(4-aminophenoxy)-2-pyridine-(N-(methyl-d3))carboxamide in dichloromethane T=20°C; 18 h;
参考文献
EP2548867 A1, ;
Paragraph 0075; 0076 ;
反应条件
in dichloromethane; dimethyl sulfoxide T=20°C; 0.333333 h; Inert atmosphere;
参考文献
EP2548867 A1, ;
Paragraph 0081; 0082 ;
反应条件
in dichloromethane T=20°C; 18 h;
参考文献
US2013/12548 A1, ;
Paragraph 0127-0129 ;