1,2,3,4-四氢异喹啉合成路线 （共 340 条）
反应条件
potassium carbonate in acetonitrile
T=60°C; 18 h;
参考文献
Proximagen Limited; Savory, Edward Daniel; Stewart, Allson; Cartey, Allison; Brown, Giles; Simpson, Iain; Oliver, Kathryn; Patient, Lee; Higginbottom, Michael; Cole, Andrew Graham
Patent: US2013/289020 A1, 2013 ;
Location in patent: Paragraph 0357 ;
参考文献
Lazewska, Dorota; Kuder, Kamil; Ligneau, Xavier; Schwartz, Jean-Charles; Schunack, Walter; Stark, Holger; Kiec-Kononowicz, Katarzyna
Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 18 p. 8729 - 8736
反应条件
1: acetic acid / 96 h / 80 °C
2: lithium aluminium tetrahydride / tetrahydrofuran / 0 - 20 °C
View Scheme
参考文献
Mathis, Cheryl L.; Gist, Brandi M.; Frederickson, Conerd K.; Midkiff, Katie M.; Marvin, Christopher C.
Tetrahedron Letters, 2013 , vol. 54, # 16 p. 2101 - 2104
反应条件
benzene
nachfolgend Verseifung mit waessrig-alkoholischer Kalilauge;
参考文献
v. Braun; Braunsdorf; Raeth
Chemische Berichte, 1922 , vol. 55, p. 1679
反应条件
1: 91 percent / Et3N / diethyl ether / 6 h / Heating
2: 1) n-BuLi / 1) THF, -78 deg C, 1 h; 2) -78 deg C, 2 h, then room t.
3: 66 percent / 2.06 M HCl / methanol / 49 h / Heating
View Scheme
参考文献
Seebach, Dieter; Lohmann, Jean-Jacques; Syfrig, Max A.; Yoshifuji, Masaaki
Tetrahedron, 1983 , vol. 39, # 12 p. 1963 - 1974
反应条件
1: diethyl ether
2: 83 percent / HgO/EDTA / aq. ethanol
3: acetic anhydride / 12 h / Ambient temperature
View Scheme
参考文献
Mohrle; Grimm
Archiv der Pharmazie, 1986 , vol. 319, # 9 p. 774 - 787
反应条件
1: With 1,8-diazabicyclo[5.4.0]undec-7-ene in acetonitrile
P=760.051 Torr; 0.75 h;
2: With tributylphosphine; di-tert-butylazodicarboxylate in acetonitrile
Mitsunobu reaction; Inert atmosphere;
参考文献
Peterson, Scott L.; Stucka, Sabrina M.; Dinsmore, Christopher J.
Organic Letters, 2010 , vol. 12, # 6 p. 1340 - 1343
反应条件
in toluene
T=0°C; Inert atmosphere;
参考文献
Allen, Julia M.; Lambert, Tristan H.
Journal of the American Chemical Society, 2011 , vol. 133, # 5 p. 1260 - 1262
反应条件
caesium carbonate in DMF (N,N-dimethyl-formamide)
T=20°C; 4 h;
参考文献
PFIZER INC.
Patent: WO2004/63198 A1, 2004 ;
Location in patent: Page 208-209 ;
WO 2004/063198 A1
反应条件
sodium carbonate in tetrahydrofuran
T=20°C; 24 h;
参考文献
Guo, Song; Zhang, Hongli; Huang, Ling; Guo, Zhendong; Xiong, Guang; Zhao, Jianzhang
Chemical Communications, 2013 , vol. 49, # 77 p. 8689 - 8691
