4-溴-2-氟-N,N-二甲基苯甲酰胺合成路线 (共 7 条)
反应条件
1: 4-Bromo-2-fluorobenzoic acid With oxalyl dichloride; N,N-dimethyl-formamide in dichloromethane T=20°C; 0.5 h; 2: dimethyl amine With triethylamine in dichloromethane T=20°C; 0.166667 h; 3: With hydrogenchloride in dichloromethane; water T=20°C;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2006/64251 A1, 2006 ;
Location in patent: Page/Page column 62-63 ;
WO 2006/064251 A1
反应条件
benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine in acetonitrile T=70°C; 2 h;
参考文献
Zhu, Jason; Razler, Thomas M.; Xu, Zhongmin; Conlon, David A.; Sortore, Eric W.; Fritz, Alan W.; Demerzhan, Roman; Sweeney, Jason T.
Organic Process Research and Development, 2011 , vol. 15, # 2 p. 438 - 442
反应条件
caesium carbonate in tetrahydrofuran
参考文献
CROWN BIOSCIENCE INC. (TAICANG); ZHONG, Boyu; SHIH, Chuan; YUAN, Hongbin; ZHOU, Feng
Patent: WO2014/32498 A1, 2014 ;
Location in patent: Page/Page column 10 ;
反应条件
1: thionyl chloride / 12 h / 20 °C 2: caesium carbonate / tetrahydrofuran View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 18, # 24 p. 6486 - 6489
反应条件
1: With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate; 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl-4',4',5',5'-tetramethyl-1,3,2-dioxaborolane in 2-methyl tetrahydrofuran
T=80°C; 15 h;
2: With water; sodium hydroxide in 2-methyl tetrahydrofuran
3: With hydrogenchloride; sodium periodate in 2-methyl tetrahydrofuran; water
T=20°C; 15 h;
参考文献
Zhu, Jason; Razler, Thomas M.; Xu, Zhongmin; Conlon, David A.; Sortore, Eric W.; Fritz, Alan W.; Demerzhan, Roman; Sweeney, Jason T.
Organic Process Research and Development, 2011 , vol. 15, # 2 p. 438 - 442
反应条件
1: With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate in 2-methyl tetrahydrofuran
T=80°C; 15 h;
2: With water; sodium hydroxide in 2-methyl tetrahydrofuran
3: With hydrogenchloride in 2-methyl tetrahydrofuran; water
T=0°C; pH=1.5;
参考文献
Zhu, Jason; Razler, Thomas M.; Xu, Zhongmin; Conlon, David A.; Sortore, Eric W.; Fritz, Alan W.; Demerzhan, Roman; Sweeney, Jason T.
Organic Process Research and Development, 2011 , vol. 15, # 2 p. 438 - 442