2-苄基-2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚合成路线 (共 11 条)
反应条件
palladium 10 on activated carbon; hydrogen in ethanol; water T=70°C; P=760.051 Torr; 24 h;
参考文献
Kalin, Jay H.; Butler, Kyle V.; Akimova, Tatiana; Hancock, Wayne W.; Kozikowski, Alan P.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 2 p. 639 - 651
反应条件
1: palladium 10 on activated carbon; hydrogen / ethanol; water / 24 h / 70 °C / 760.05 Torr
2: tetrahydrofuran / 8 h / Inert atmosphere; Reflux
View Scheme
参考文献
Kalin, Jay H.; Butler, Kyle V.; Akimova, Tatiana; Hancock, Wayne W.; Kozikowski, Alan P.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 2 p. 639 - 651
反应条件
sulfuric acid in 1,4-dioxane; water
18 h; Reflux;
参考文献
AMGEN INC.; BREGMAN, Howard; BUCHANAN, John, L.; CHAKKA, Nagasree; DIMAURO, Erin, F.; DU, Bingfan; NGUYEN, Hanh, Nho; ZHENG, Xiao, Mei
Patent: WO2011/103196 A1, 2011 ;
Location in patent: Page/Page column 83 ;
WO 2011/103196 A1
反应条件
sodium amide; sodium t-butanolate in tetrahydrofuran
T=55 - 60°C; Fischer Indole Synthesis; 24 h; Inert atmosphere;
参考文献
USTAV EXPIREMENTALNEJ FARMAKOLOGIE A TOXIKOLOGIE SAV; SNIRC, Vladimir; BUCHMAN, Marek; STEFEK, Milan; BAUER, Viktor; STOLC, Svorad; MIHALOVA, Danica; PATOPRSTY, Vladimir; POVAZANEC, Frantisek
Patent: WO2011/139242 A2, 2011 ;
Location in patent: Page/Page column 12-13 ;
反应条件
lithium diisopropyl amide in tetrahydrofuran; cyclohexane
5 h; Heating;
参考文献
Kudzma, Linas V.
Synthesis, 2003 , # 11 p. 1661 - 1666
反应条件
1: 92 percent / p-TsOH / toluene / 15 h / Heating
2: 97 percent / LDA*THF / tetrahydrofuran; cyclohexane / 5 h / Heating
View Scheme
参考文献
Kudzma, Linas V.
Synthesis, 2003 , # 11 p. 1661 - 1666
反应条件
1: 92 percent / p-TsOH / toluene / 15 h / Heating
2: 97 percent / LDA*THF / tetrahydrofuran; cyclohexane / 5 h / Heating
View Scheme
参考文献
Kudzma, Linas V.
Synthesis, 2003 , # 11 p. 1661 - 1666
反应条件
1: 86 percent / propan-2-ol / Heating
2: 88 percent / NaBH4 / aq. ethanol / 20 °C
View Scheme
参考文献
Smolyar; Volchkov; Yutilov
Pharmaceutical Chemistry Journal, 2001 , vol. 35, # 9 p. 514 - 517
反应条件
1: 99 percent / paraffin / 0.67 h / 320 - 350 °C
2: 86 percent / propan-2-ol / Heating
3: 88 percent / NaBH4 / aq. ethanol / 20 °C
View Scheme
参考文献
Smolyar; Volchkov; Yutilov
Pharmaceutical Chemistry Journal, 2001 , vol. 35, # 9 p. 514 - 517
反应条件
Fischer indole synthesis; Acidic conditions;
参考文献
Bridoux, Alexandre; Millet, Regis; Pommery, Jean; Pommery, Nicole; Henichart, Jean-Pierre
Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 11 p. 3910 - 3924