3-苯磺酰基-8-(哌嗪-1-基)喹啉合成路线 (共 7 条)
反应条件
sodium t-butanolate; 1,1'-bis-(diphenylphosphino)ferrocene; tris-(dibenzylideneacetone)dipalladium(0) in 1,4-dioxane T=40°C; 16.5 h;
参考文献
GLAXO GROUP LIMITED
Patent: WO2005/26125 A1, 2005 ;
Location in patent: Page/Page column 21-22 ;
WO 2005/026125 A1
反应条件
potassium carbonate in propan-1-ol T=100°C; 17.25 - 23 h; Product distribution / selectivity;
参考文献
GLAXO GROUP LIMITED
Patent: WO2007/39238 A1, 2007 ;
Location in patent: Page/Page column 14-16 ;
反应条件
palladium diacetate; sodium t-butanolate; dicyclohexyl(2',6'-diisopropoxy-[1,1'-biphenyl]-2-yl)phosphine in 1,4-dioxane T=90°C; Buchwald-Hartwig Coupling; 16 h; Inert atmosphereSchlenk technique;
参考文献
Emmett, Edward J.; Hayter, Barry R.; Willis, Michael C.
Angewandte Chemie - International Edition, 2013 , vol. 52, # 48 p. 12679 - 12683
Angew. Chem., 2013 , vol. 125, # 48 p. 12911 - 12915,5
反应条件
1: N-methyl-2-(methylamino)ethylamine; caesium carbonate; copper(l) iodide / dimethyl sulfoxide / 4 h / 110 °C 2: tris-(dibenzylideneacetone)dipalladium(0); N-[2'-(dicyclohexylphosphino)-1,1'-biphenyl-2-yl]-N,N-dimethylamine; sodium t-butanolate / toluene / 110 °C / |Inert atmosphere 3: trifluoroacetic acid / dichloromethane / 2 h View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890
反应条件
1: tris-(dibenzylideneacetone)dipalladium(0); N-[2'-(dicyclohexylphosphino)-1,1'-biphenyl-2-yl]-N,N-dimethylamine; sodium t-butanolate / toluene / 110 °C / |Inert atmosphere 2: trifluoroacetic acid / dichloromethane / 2 h View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890
反应条件
1: N-iodo-succinimide; acetic acid; sodium sulfite / 1 h / 20 - 80 °C 2: N-methyl-2-(methylamino)ethylamine; caesium carbonate; copper(l) iodide / dimethyl sulfoxide / 4 h / 110 °C 3: tris-(dibenzylideneacetone)dipalladium(0); N-[2'-(dicyclohexylphosphino)-1,1'-biphenyl-2-yl]-N,N-dimethylamine; sodium t-butanolate / toluene / 110 °C / |Inert atmosphere 4: trifluoroacetic acid / dichloromethane / 2 h View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890
反应条件
trifluoroacetic acid in dichloromethane 2 h;
参考文献
Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890