3-氨基-1-(3-三氟甲基苯基)吡唑合成路线 （共 4 条）
反应条件
hydrogen; palladium on activated charcoal in methanol
T=20°C;
参考文献
ARDELYX, INC.; LEWIS, Jason, G.; JACOBS, Jeffrey, W.; REICH, Nicholas; LEADBETTER, Michael, R.; BELL, Noah; CHANG, Han-Ting; CHEN, Tao; NAVRE, Marc; CHARMOT, Dominique; CARRERAS, Christopher; LABONTE, Eric
Patent: WO2012/6473 A1, 2012 ;
Location in patent: Page/Page column 70 ;
WO 2012/006473 A1
反应条件
N-bromosuccinmide in toluene
1 h; Reflux;
参考文献
GLENMARK PHARMACEUTICALS S.A.; KUMAR, Sukkeerthi; THOMAS, Abraham; WAGHMARE, Nayan, Taterao; KHAIRATKAR-JOSHI, Neelima; MUKHOPADHYAY, Indranil
Patent: WO2011/132017 A1, 2011 ;
Location in patent: Page/Page column 24-25 ;
WO 2011/132017 A1
反应条件
1: potassium carbonate; L-proline; copper(l) iodide / dimethyl sulfoxide / 85 °C
2: hydrogen / palladium on activated charcoal / methanol / 20 °C
View Scheme
参考文献
ARDELYX, INC.; LEWIS, Jason, G.; JACOBS, Jeffrey, W.; REICH, Nicholas; LEADBETTER, Michael, R.; BELL, Noah; CHANG, Han-Ting; CHEN, Tao; NAVRE, Marc; CHARMOT, Dominique; CARRERAS, Christopher; LABONTE, Eric
Patent: WO2012/6473 A1, 2012 ;
WO 2012/006473 A1
反应条件
1: sodium ethanolate / ethanol / 24 h / Reflux
2: N-bromosuccinmide / toluene / 1 h / Reflux
View Scheme
参考文献
GLENMARK PHARMACEUTICALS S.A.; KUMAR, Sukkeerthi; THOMAS, Abraham; WAGHMARE, Nayan, Taterao; KHAIRATKAR-JOSHI, Neelima; MUKHOPADHYAY, Indranil
Patent: WO2011/132017 A1, 2011 ;
WO 2011/132017 A1
