3-氨基-5-氟三氟甲基苯合成路线 (共 7 条)
反应条件
hydrogen; triethylamine; palladium 10 on activated carbon in ethanol T=20 - 25°C; 20 h;
参考文献
NOVARTIS AG; NOVARTIS PHARMA GmbH
Patent: WO2006/135640 A2, 2006 ;
Location in patent: Page/Page column 10; 18-19 ;
反应条件
hydrazine hydrate; nickel Reduction;
参考文献
Mishani; Bonasera; Rozen; Ortu; Gazit; Levitzki
Journal of Labelled Compounds and Radiopharmaceuticals, 1999 , vol. 42, # SUPPL. 1 p. S27-S29
反应条件
1: fluoride ion 2: hydrazine hydrate / Raney nickel View Scheme
参考文献
Mishani; Bonasera; Rozen; Ortu; Gazit; Levitzki
Journal of Labelled Compounds and Radiopharmaceuticals, 1999 , vol. 42, # SUPPL. 1 p. S27-S29
反应条件
hydrogenchloride in diethyl ether; toluene
参考文献
NOVO NORDISK A/S; AGOURON PHARMACEUTICALS, INC.
Patent: EP1183229 B1, 2005 ;
Location in patent: Page/Page column 158 ;
反应条件
1: With hydrogenchloride; trifluoroacetic acid; sodium nitrite in water T=0°C; 2: With sulfur dioxide; anhydrous sulfurous acid; acetic acid; copper(l) chloride; copper dichloride in water T=0 - 20°C;
参考文献
Blanc, Jean-Baptiste; Chen, Li; Firooznia, Fariborz; Gillespie, Paul; Goodnow, JR., Robert Alan; Lin, Tai-An; Pan, Song; So, Sung-Sau; Yun, HongYing
Patent: US2010/41760 A1, 2010 ;
Location in patent: Page/Page column 22 ;
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
NOVARTIS AG; NOVARTIS PHARMA GmbH
Patent: WO2006/135640 A2, 2006 ;
Location in patent: Page/Page column 19 ;
参考文献
BRISTOL-MYERS SQUIBB COMPANY
Patent: WO2009/3077 A1, 2008 ;
Location in patent: Page/Page column 132 ;