3-溴-1,1,1-三氟丙酮合成路线 (共 31 条)
反应条件
bromine in sulfuric acid 2 h; Ambient temperature;
参考文献
Moazzam, Muhammad; Parrick, J.
Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry, 1988 , vol. 27, # 1-12 p. 1051 - 1053
反应条件
(i) aq. HBr, (ii) (heating); Multistep reaction;
参考文献
Cherbuliez,E. et al.
Helvetica Chimica Acta, 1965 , vol. 48, p. 1423 - 1426
反应条件
in tert-butyl alcohol 8 h; Reflux;
参考文献
Vieira, Eric; Huwyler, Joerg; Jolidon, Synese; Knoflach, Frederic; Mutel, Vincent; Wichmann, Juergen
Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 6 p. 1666 - 1669
反应条件
1: in ethanol T=50°C; 2 h; 2: With sodium hydroxide; water pH=> 12;
参考文献
ELI LILLY AND COMPANY
Patent: WO2008/36579 A1, 2008 ;
Location in patent: Page/Page column 43 ;
WO 2008/036579 A1
反应条件
1: T=140°C; 2.5 h; Neat (no solvent); 2: With potassium carbonate in water T=20°C;
参考文献
AMGEN INC.; ZENG, Qingping; YUAN, Chester Chenguang; YAO, Guomin; WANG, Xianghong; TADESSE, Seifu; ST. JEAN, JR., David J.; REICHELT, Andreas; LIU, Qingyian; HONG, Fang-Tsao; HAN, Nianhe; FOTSCH, Christopher H.; DAVIS, Carl D.; BOURBEAU, Matthew P.; ASHTON, Kate S.; ALLEN, John G.
Patent: WO2010/83246 A1, 2010 ;
Location in patent: Page/Page column 100 ;
参考文献
Moazzam, Muhammad; Parrick, J.
Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry, 1988 , vol. 27, # 1-12 p. 1051 - 1053
反应条件
1: 4-[1-methyl-2-(4-(trifluoromethyl)phenylamino)-1H-benzoimidazol-5-yloxy]-pyridine-2-carbonitrile With sodium methylate in isopropyl alcohol T=50°C; 1 h; 2: 3-bromo-1,1,1-trifluoroacetone With ammonium acetate in isopropyl alcohol T=70 - 85°C; 23 h; Product distribution / selectivity;
参考文献
Novartis AG
Patent: US2007/49622 A1, 2007 ;
Location in patent: Page/Page column 44 ;
反应条件
1: in ethanol 18 h; Heating / reflux; 2: With methanol; 1,8-diazabicyclo[5.4.0]undec-7-ene in ethanol T=20°C; 48 h;
参考文献
MERCK SHARP and DOHME LIMITED; HOLLINGWORTH, Gregory, John; JONES, A., Brian; SPAREY, Timothy, Jason
Patent: WO2005/49613 A1, 2005 ;
Location in patent: Page/Page column 52 ;
WO 2005/049613 A1
反应条件
sodium hydrogencarbonate in dichloromethane
参考文献
The Regents of the University of California
Patent: US4562292 A1, 1985 ;
反应条件
1: in 1,4-dioxane; ethanol 2: With triethylamine in 1,4-dioxane; ethanol Reflux;
参考文献
Vilchis-Reyes, Miguel Angel; Zentella, Alejandro; Martinez-Urbina, Miguel Angel; Guzman, Angel; Vargas, Omar; Ramirez Apan, Maria Teresa; Ventura Gallegos, Jose Luis; Diaz, Eduardo
European Journal of Medicinal Chemistry, 2010 , vol. 45, # 1 p. 379 - 386