1,3,4,5-四氢-苯并[B][1,4]二氮杂革-2-酮合成路线 (共 13 条)
反应条件
sodium in methanol T=0 - 20°C;
参考文献
CONSTELLATION PHARMACEUTICALS, INC.; ALBRECHT, Brian, K.; GEHLING, Victor, S.; HEWITT, Michael, C.; TAYLOR, Alexander, M.; HARMANGE, Jean-Christophe
Patent: WO2012/151512 A2, 2012 ;
Location in patent: Page/Page column 113-114 ;
反应条件
hydrogenchloride in ethanol; water T=70°C; 3 h;
参考文献
Baraldi, Pier Giovanni; Ruggiero, Emanuela; Tabrizi, Mojgan Aghazadeh
Journal of Heterocyclic Chemistry, 2014 , vol. 51, # 1 p. 101 - 105
反应条件
copper(l) iodide; potassium carbonate; N-methyl-2-(methylamino)ethylamine in toluene T=110°C; 22 h;
参考文献
Journal of the American Chemical Society, , vol. 126, # 11 p. 3529 - 3533
反应条件
titanium(IV) isopropylate in toluene T=110°C; 24 h;
参考文献
Klapars, Artis; Parris, Sean; Anderson, Kevin W.; Buchwald, Stephen L.
Journal of the American Chemical Society, 2004 , vol. 126, # 11 p. 3529 - 3533
反应条件
1: 3-azidopropanoic acid With triethylamine; diisopropyl-carbodiimide in N,N-dimethyl-formamide T=25°C; 0.0833333 h; 2: para-phenylenediamine hydrochloride in N,N-dimethyl-formamide T=25°C; 5 h; Inert atmosphereDarkness;
参考文献
Doebelin, Christelle; Schmitt, Martine; Antheaume, Cyril; Bourguignon, Jean-Jacques; Bihel, Frederic
Journal of Organic Chemistry, 2013 , vol. 78, # 22 p. 11335 - 11341
反应条件
potassium phosphate; copper(l) iodide; N-methyl-2-(methylamino)ethylamine in toluene T=100°C; 5 h;
参考文献
Journal of the American Chemical Society, , vol. 126, # 11 p. 3529 - 3533
参考文献
US5536718 A1, ;
US 5536718 A
反应条件
1: hydrogen / palladium 10 on activated carbon / ethyl acetate; methanol / 20 °C 2: sodium / methanol / 0 - 20 °C View Scheme
反应条件
sodium azide; sulfuric acid 24 h; Ambient temperature; Title compound not separated from byproducts;
参考文献
Journal of Medicinal Chemistry, , vol. 39, # 18 p. 3539 - 3546
反应条件
1: 67 percent / NaHCO3 2: 67 percent / P2S5 / pyridine / 4 h / 80 °C View Scheme
参考文献
Puodziunaite; Kosychova; Janciene; Stumbreviciute
Monatshefte fur Chemie, 1997 , vol. 128, # 12 p. 1275 - 1281