1,2-二氢-4-羟基-1-甲基-2-氧代-3-喹啉羧酸合成路线 （共 8 条）
反应条件
dicyclohexyl-carbodiimide in toluene T=80 - 85°C; 2 h; Large scale; Concentration;
参考文献
Sjoevall, Sven; Hansen, Lars; Granquist, Bo
Organic Process Research and Development, 2004 , vol. 8, # 5 p. 802 - 807
反应条件
hydrogen; palladium on activated charcoal in ethyl acetate
P=735.5 Torr; 0.166667 h;
参考文献
Coppola, Gary M.; Damon, Robert E.; Hardtmann, Goetz E.
Synthesis, 1981 , # 5 p. 391 - 392
反应条件
hydrogenchloride; acetic acid
T=80 - 85°C; 2 h; Large scale;
参考文献
Sjoevall, Sven; Hansen, Lars; Granquist, Bo
Organic Process Research and Development, 2004 , vol. 8, # 5 p. 802 - 807
反应条件
1: 90 percent / Sodium hydride / N,N-dimethyl-acetamide / 1.5 h / 115 °C
2: 75 percent / Perchloric acid / acetonitrile / 0.01 h / ice cooled
View Scheme
参考文献
Coppola, Gary M.; Damon, Robert E.; Hardtmann, Goetz E.
Synthesis, 1981 , # 5 p. 391 - 392
反应条件
perchloric acid in acetonitrile
0.00833333 h; ice cooled;
参考文献
Coppola, Gary M.; Damon, Robert E.; Hardtmann, Goetz E.
Synthesis, 1981 , # 5 p. 391 - 392
反应条件
hydrogenchloride
5 h; Heating;
参考文献
Ukrainets, I.V.; Gorokhova, O.V.; Taran, S.G.; Bezuglyi, P.A.; Turov, A.V.; et al.
Chemistry of Heterocyclic Compounds (New York, NY, United States), 1994 , vol. 30, # 7 p. 829 - 836
Khimiya Geterotsiklicheskikh Soedinenii, 1994 , # 7 p. 958 - 966
反应条件
1: Et3N / CH2Cl2 / 8 h / Ambient temperature
2: aq. KOH / 5 h
3: 96 percent / aq. HCl / 1 h
4: 89 percent / 2N aq. HCl / 5 h / Heating
View Scheme
参考文献
Ukrainets, I.V.; Gorokhova, O.V.; Taran, S.G.; Bezuglyi, P.A.; Turov, A.V.; et al.
Chemistry of Heterocyclic Compounds (New York, NY, United States), 1994 , vol. 30, # 7 p. 829 - 836
Khimiya Geterotsiklicheskikh Soedinenii, 1994 , # 7 p. 958 - 966
反应条件
1.1: potassium carbonate / N,N-dimethyl-formamide / 1 h / 0 - 30 °C
2.1: sodium methylate / N,N-dimethyl-formamide / 25 - 85 °C / Inert atmosphere
2.2: 0.5 h / 80 - 85 °C / Inert atmosphere
2.3: 25 - 30 °C / pH 1
3.1: hydrogenchloride; acetic acid / 2 h / 80 - 85 °C
View Scheme
参考文献
ACTAVIS GROUP PTC EHF
Patent: US2012/9226 A1, 2012 ;
