8-硝基-2,3-二氢-4(1H)-喹啉酮合成路线 （共 5 条）
反应条件
sodium azide; methanesulfonic acid Schmidt reaction;
参考文献
Skalitzky, Donald J.; Marakovits, Joseph T.; Maegley, Karen A.; Ekker, Anne; Yu, Xiao-Hong; Hostomsky, Zdenek; Webber, Stephen E.; Eastman, Brian W.; Almassy, Robert; Li, Jianke; Curtin, Nicola J.; Newell, David R.; Calvert, A. Hilary; Griffin, Roger J.; Golding, Bernard T.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 2 p. 210 - 213
反应条件
methanesulfonic acid; phosphorus pentoxide
T=70 - 80°C; 1.5 h;
参考文献
Skalitzky, Donald J.; Marakovits, Joseph T.; Maegley, Karen A.; Ekker, Anne; Yu, Xiao-Hong; Hostomsky, Zdenek; Webber, Stephen E.; Eastman, Brian W.; Almassy, Robert; Li, Jianke; Curtin, Nicola J.; Newell, David R.; Calvert, A. Hilary; Griffin, Roger J.; Golding, Bernard T.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 2 p. 210 - 213
反应条件
1: 95 percent / aq. NaOH / methanol / 3.5 h / Heating
2: 46 percent / P2O5; MeSO3H / 1.5 h / 70 - 80 °C
View Scheme
参考文献
Skalitzky, Donald J.; Marakovits, Joseph T.; Maegley, Karen A.; Ekker, Anne; Yu, Xiao-Hong; Hostomsky, Zdenek; Webber, Stephen E.; Eastman, Brian W.; Almassy, Robert; Li, Jianke; Curtin, Nicola J.; Newell, David R.; Calvert, A. Hilary; Griffin, Roger J.; Golding, Bernard T.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 2 p. 210 - 213
反应条件
1: 79 percent / Triton B / dioxane; methanol / 1 h
2: 95 percent / aq. NaOH / methanol / 3.5 h / Heating
3: 46 percent / P2O5; MeSO3H / 1.5 h / 70 - 80 °C
View Scheme
参考文献
Skalitzky, Donald J.; Marakovits, Joseph T.; Maegley, Karen A.; Ekker, Anne; Yu, Xiao-Hong; Hostomsky, Zdenek; Webber, Stephen E.; Eastman, Brian W.; Almassy, Robert; Li, Jianke; Curtin, Nicola J.; Newell, David R.; Calvert, A. Hilary; Griffin, Roger J.; Golding, Bernard T.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 2 p. 210 - 213
反应条件
hydrogen; palladium 10 on activated carbon in methanol
P=760.051 Torr; 16 h;
参考文献
ALTANA PHARMA AG
Patent: WO2004/108723 A1, 2004 ;
Location in patent: Page 14 ;
