3-(4-甲基-1H-咪唑-1-基)-5-(三氟甲基)苯胺合成路线 （共 9 条）
反应条件
hydrogen; 5 palladium over charcoal in ethanol T=70°C; P=3000.3 Torr; 3 h; Product distribution / selectivity;
参考文献
NOVARTIS AG; NOVARTIS PHARMA GmbH
Patent: WO2006/135640 A2, 2006 ;
Location in patent: Page/Page column 23 ;
反应条件
potassium phosphate; tris-(dibenzylideneacetone)dipalladium(0) in toluene; tert-butyl alcohol T=120°C; 8 h; Inert atmosphere;
参考文献
Guangzzhou Institute of Biomedicine and Health, Chineses Academy of Sciences; Ding, Ke; Wang, Deping; Pei, Duanqing; Zhang, Zhang; Shen, Mengjie; Luo, Kun; Feng, Yubing
Patent: US2013/196985 A1, 2013 ;
Location in patent: Paragraph 0125-0128 ;
反应条件
potassium hydrogencarbonate in ethanol; water T=0 - 45°C; 3.5 h; Product distribution / selectivity;
参考文献
NOVARTIS AG; NOVARTIS PHARMA GmbH
Patent: WO2006/135640 A2, 2006 ;
Location in patent: Page/Page column 21 ;
反应条件
1: 4-methyl-1H-imidazole With sodium hydride in tetrahydrofuran T=20 - 25°C; 0.25 h; 2: 3-fluoro-5-(trifluoromethyl)aniline in tetrahydrofuran; 1-methyl-pyrrolidin-2-one T=20 - 165°C; 22.25 h; Product distribution / selectivity;
参考文献
WO2006/135640 A2, ;
Page/Page column 19 ;
反应条件
4-(N,N-dimethlyamino)pyridine; N-ethyl-N,N-diisopropylamine in tetrahydrofuran T=20°C; 2 h;
参考文献
Huang, Wei-Sheng; Shakespeare, William C.
Synthesis, 2007 , # 14 p. 2121 - 2124
反应条件
1: 3-Iodo-4-methyl-benzoic acid With thionyl chloride 1 h; Heating / reflux; 2: 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzeneamine With N-ethyl-N,N-diisopropylamine; 4-(N,N-dimethlyamino)pyridine in tetrahydrofuran; benzene T=20°C; 2 h;
参考文献
ARIAD PHARMACEUTICALS, INC.
Patent: WO2007/21937 A2, 2007 ;
Location in patent: Page/Page column 38 ;
反应条件
4-(N,N-dimethlyamino)pyridine; N-ethyl-N,N-diisopropylamine in tetrahydrofuran; thionyl chloride; water
参考文献
Astar Biotech LLC; YU, Chunrong; Huang, Haihong; Zhang, Dongfeng; Li, Peng
Patent: US2014/31354 A1, 2014 ;
Location in patent: Paragraph 0293; 0396; 0397 ;
反应条件
potassium tert-butylate in tetrahydrofuran T=0 - 20°C; 12 h; Inert atmosphere;
参考文献
Journal of the American Chemical Society, , vol. 134, # 1 p. 700 - 706
反应条件
1: 4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]benzoic acid With thionyl chloride in 1-methyl-pyrrolidin-2-one T=60°C; 1.25 h; 2: 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzeneamine in 1-methyl-pyrrolidin-2-one T=90°C; 3 h; Product distribution / selectivity;
参考文献
US2010/16590 A1, ;
Page/Page column 20 ;
