1,2,3,4-四氢-2-甲基-7-异喹啉胺合成路线 （共 11 条）
反应条件
hydrogen; palladium on activated charcoal in methanol
Reduction;
参考文献
Chan, Wai N.; Hadley, Michael S.; Harling, John D.; Herdon, Hugh J.; Orlek, Barry S.; Riley, Graham J.; Stead, Rachel E. A.; Stean, Tania O.; Thompson, Mervyn; Upton, Neil; Ward, Robert W.
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 8 p. 2085 - 2094
反应条件
1: With lithium aluminium tetrahydride in tetrahydrofuran
T=-5°C; 12 h; Heating / reflux;
2: With water; Sodium potassium tartrate in tetrahydrofuran
T=20°C; 3 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
Patent: WO2007/48802 A1, 2007 ;
Location in patent: Page/Page column 93 ;
反应条件
1: 1.7 g / 88 percent formic acid / H2O / 2 h / 80 °C
2: 99 percent / H2 / 10 percent Pd/C / methanol
View Scheme
参考文献
Chan, Wai N.; Hadley, Michael S.; Harling, John D.; Herdon, Hugh J.; Orlek, Barry S.; Riley, Graham J.; Stead, Rachel E. A.; Stean, Tania O.; Thompson, Mervyn; Upton, Neil; Ward, Robert W.
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 8 p. 2085 - 2094
反应条件
1: 86 percent / conc. H2SO4 / acetic acid / 20 h / 25 °C
2: 11 g / K2CO3 / methanol; H2O / 18 h
3: 1.7 g / 88 percent formic acid / H2O / 2 h / 80 °C
4: 99 percent / H2 / 10 percent Pd/C / methanol
View Scheme
参考文献
Chan, Wai N.; Hadley, Michael S.; Harling, John D.; Herdon, Hugh J.; Orlek, Barry S.; Riley, Graham J.; Stead, Rachel E. A.; Stean, Tania O.; Thompson, Mervyn; Upton, Neil; Ward, Robert W.
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 8 p. 2085 - 2094
反应条件
1: 11 g / K2CO3 / methanol; H2O / 18 h
2: 1.7 g / 88 percent formic acid / H2O / 2 h / 80 °C
3: 99 percent / H2 / 10 percent Pd/C / methanol
View Scheme
参考文献
Chan, Wai N.; Hadley, Michael S.; Harling, John D.; Herdon, Hugh J.; Orlek, Barry S.; Riley, Graham J.; Stead, Rachel E. A.; Stean, Tania O.; Thompson, Mervyn; Upton, Neil; Ward, Robert W.
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 8 p. 2085 - 2094
反应条件
1.1: sodium hydroxide / water; 1,2-dichloro-ethane / 0.17 h
1.2: 16 h / 90 °C
1.3: 1 h / 20 °C
2.1: hydrogen / palladium 10 on activated carbon / ethyl acetate / 16 h / 20 °C / 1551.49 Torr
View Scheme
参考文献
ABBOTT LABORATORIES; BA-MAUNG, Nwe Y.; CLARK, Richard F.; ERICKSON, Scott A.; FIDANZE, Steve D.; KAWAI, Megumi; MANTEI, Robert A.; SHEPPARD, George S.; SORENSON, Bryan K.; WANG, Gary T.
Patent: WO2011/53476 A1, 2011 ;
WO 2011/053476 A1
反应条件
1.1: sodium nitrate; sulfuric acid / 4 - 20 °C
1.2: pH 8
2.1: water; sodium tris(acetoxy)borohydride / 1,2-dichloro-ethane / 24 h / 20 °C
3.1: hydrogen / palladium 10 on activated carbon / ethanol; water / 24 h / 20 °C / 760.05 Torr
View Scheme
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; COOK, Brian Nicholas; KOWALSKI, Jennifer A.; LI, Xiang; MARSHALL, Daniel Richard; SCHLYER, Sabine; SIBLEY, Robert; SMITH-KEENAN, Lana Louise; SOLEYMANZADEH, Fariba; SORCEK, Ronald John; YOUNG, Erick Richard Roush; ZHANG, Yunlong
Patent: WO2012/6203 A1, 2012 ;
WO 2012/006203 A1
反应条件
sulfuric acid; nitric acid
Hydrierung des Reaktionsprodukts an Palladium/Kohle in Aethanol;
参考文献
Ochiai; Nakagome
Chemical and Pharmaceutical Bulletin, 1958 , vol. 6, p. 497,500
反应条件
2: Raney nickel; ethanol / Hydrogenation
View Scheme
参考文献
Lusinchi et al.
Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1959 , vol. 248, p. 426
反应条件
potassium hydrogencarbonate in sodium carbonate; benzene
参考文献
Marion Laboratories, Inc.
Patent: US4022900 A1, 1977 ;
