2,4,5-三氟-3-甲氧基苯甲酰氯合成路线 (共 17 条)
反应条件
thionyl chloride 2 h; Reflux;
参考文献
Chen, Yin-Bo; Li, Ji-Ling; Shao, Xu-Sheng; Xu, Xiao-Yong; Li, Zhong
Chinese Chemical Letters, 2013 , vol. 24, # 8 p. 673 - 676
反应条件
1: aq. NaOH / methanol 2: (COCl)2; DMF / CH2Cl2 View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 47, # 19 p. 4693 - 4709
反应条件
1: 1.88 g / Et3N / toluene / 5 h / 90 °C 2: ethanol; diethyl ether / 3 h / 20 °C 3: 627 mg / K2CO3 / dimethylformamide / 5 h / 100 °C View Scheme
参考文献
Sanchez, Joseph P.; Gogliotti, Rocco D.; Domagala, John M.; Gracheck, Stephen J.; Huband, Michael D.; et al.
Journal of Medicinal Chemistry, 1995 , vol. 38, # 22 p. 4478 - 4487
反应条件
[2,2']bipyridinyl; n-butyllithium 1.) THF, hexane, from -20 deg C to -5 deg C, 2.) THF, hexane, -30 deg C, 2 h; Yield given. Multistep reaction;
参考文献
THE PROCTER and GAMBLE COMPANY
Patent: WO2004/14893 A2, 2004 ;
Location in patent: Page 75; 76 ;
反应条件
1: diethylmalonate potassium salt With triethylamine; magnesium chloride in acetonitrile T=20 - 25°C; 2: 2,4,5-trifluoro-3-methoxybenzoic acid chloride With triethylamine in acetonitrile T=20°C; 18 h;
参考文献
Baker, William R.; Cai, Shaopei; Dimitroff, Martin; Fang, Liming; Huh, Kay K.; Ryckman, David R.; Shang, Xiao; Shawar, Ribhi M.; Therrien, Joseph H.
Journal of Medicinal Chemistry, 2004 , vol. 47, # 19 p. 4693 - 4709
反应条件
1: malonic acid ethyl ester monopotassium salt With magnesium chloride in ethyl acetate T=20°C; 0.5 h; Inert atmosphere; 2: With triethylamine in ethyl acetate T=20°C; 0.5 h; Inert atmosphere; 3: 2,4,5-trifluoro-3-methoxybenzoic acid chloride in ethyl acetate 2 h; Inert atmosphereReflux;
参考文献
Hashimoto, Akihiro; Pais, Godwin C. G.; Wang, Qiuping; Lucien, Edlaine; Incarvito, Christopher D.; Deshpande, Milind; Bradburyand, Barton J.; Wiles, Jason A.
Organic Process Research and Development, 2007 , vol. 11, # 3 p. 389 - 398
反应条件
1: triethylamine; magnesium chloride / ethyl acetate 2: hydrogenchloride; water View Scheme
参考文献
Marks, Kevin R.; Malik, Muhammad; Mustaev, Arkady; Hiasa, Hiroshi; Drlica, Karl; Kerns, Robert J.
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 15 p. 4585 - 4588
反应条件
1: ammonia / tetrahydrofuran / 1.17 h / -50 - 20 °C 2: oxalyl dichloride / 1,2-dichloro-ethane / 24 h / 20 °C / |Reflux 3: dichloromethane / -6 - 20 °C 4: sodium hydride / toluene; ethylene glycol dimethyl ether; mineral oil / 24.5 h / -4 °C / |Reflux 5: potassium carbonate / N,N-dimethyl-formamide; 1,4-dioxane / 20 h / 70 - 72 °C View Scheme
参考文献
Beylin, Vladimir; Boyles, David C.; Curran, Timothy T.; Macikenas, Dainius; Parlett IV, Roger V.; Vrieze, Derek
Organic Process Research and Development, 2007 , vol. 11, # 3 p. 441 - 449
反应条件
1: ammonia / tetrahydrofuran / 1.17 h / -50 - 20 °C 2: oxalyl dichloride / 1,2-dichloro-ethane / 24 h / 20 °C / |Reflux 3: dichloromethane / -6 - 20 °C 4: sodium hydride / toluene; ethylene glycol dimethyl ether; mineral oil / 24.5 h / -4 °C / |Reflux View Scheme
参考文献
Beylin, Vladimir; Boyles, David C.; Curran, Timothy T.; Macikenas, Dainius; Parlett IV, Roger V.; Vrieze, Derek
Organic Process Research and Development, 2007 , vol. 11, # 3 p. 441 - 449
反应条件
magnesium diethoxide in toluene T=25°C; 1 h;
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: EP1518856 A1, 2005 ;
Location in patent: Page/Page column 12 ;