4-(Boc-氨基)吡啶合成路线 （共 36 条）
反应条件
1: pyridin-4-yl-carbamic acid tert-butyl ester With n-butyllithium; N,N,N',N,-tetramethylethylenediamine in tetrahydrofuran; hexane T=-78 - -4°C; 2.5 h; Inert atmosphere; 2: boric acid trimethyl ester in tetrahydrofuran; hexane T=-78 - 0°C; 0.25 h; 3: With water; ammonium chloride in tetrahydrofuran; hexane 0.0333333 h;
参考文献
Coley Pharmaceutical Group, Inc.
Patent: US2011/269965 A1, 2011 ;
Location in patent: Page/Page column 29 ;
反应条件
tert.-butyl lithium in tetrahydrofuran; pentane 1.) -78 deg C, 15 min, -20 deg C, 1.5 h, 2.) -15 deg C to room temperature;
参考文献
Venuti, Michael C.; Stephenson, Robert A.; Alvarez, Robert; Bruno, John J.; Strosberg, Arthur M.
Journal of Medicinal Chemistry, 1988 , vol. 31, # 11 p. 2136 - 2145
参考文献
PROSIDION LIMITED
Patent: WO2006/59164 A2, 2006 ;
Location in patent: Page/Page column 37 ;
反应条件
tert.-butyl lithium in tetrahydrofuran T=-78°C;
参考文献
Chan, Laval; Jin, Haolun; Stefanac, Tomislav; Lavallee, Jean-Francois; Falardeau, Guy; Wang, Wei; Bedard, Jean; May, Suzanne; Yuen, Leonard
Journal of Medicinal Chemistry, 1999 , vol. 42, # 16 p. 3023 - 3025
反应条件
in tetrahydrofuran; water
参考文献
Warner-Lambert Company
Patent: US5654307 A1, 1997 ;
US 5654307 A
反应条件
carbon dioxide in tetrahydrofuran; pentane
参考文献
ELI LILLY AND COMPANY
Patent: EP1140905 B1, 2003 ;
反应条件
1: 1.) tBuLi / 1.) THF, hexane, -10 deg C, 3 h, 2.) THF, hexane, a) -78 deg C, 5 min, b) RT, 15 min 2: 68 percent / 0.42 h / 192 °C View Scheme
参考文献
Rivalle, Christian; Bisagni, Emile
Journal of Heterocyclic Chemistry, 1997 , vol. 34, # 2 p. 441 - 444
反应条件
1.1: dinitrogen pentoxide / nitromethane / cooling 1.2: 51 percent / aq. sodium bisulfite / methanol / 20 °C 2.1: 95 percent / hydrogen / palladium on carbon / methanol / 7500.6 Torr View Scheme
参考文献
Bakke, Jan M.; Gautun, Hanna S. H.; Svensen, Harald
Journal of Heterocyclic Chemistry, 2003 , vol. 40, # 4 p. 585 - 591
反应条件
1: 1.) BuLi / 1.) THF, hexane, 0 deg C, 3 h, 2.) THF, hexane, 20 deg C, 1 h 2: 1.) t-BuLi / 1.) THF, pentane, -40 deg C, 1 h, 2.) THF, pentane, 20 deg C, 1 h 3: 5.5 M HCl / 1 h / 45 - 50 °C View Scheme
参考文献
Hands, David; Bishop, Brian; Cameron, Mark; Edwards, John S.; Cottrell, Ian F.; Wright, Stanley H. B.
Synthesis, 1996 , # 7 p. 877 - 882
反应条件
1: With tert.-butyl lithium in tetrahydrofuran; pentane T=-78 - -15°C; Metallation; lithiation; 3.5 h; 2: With ethylene dibromide in tetrahydrofuran; pentane T=-78 - 20°C; Bromination; 2 h;
参考文献
Spivey, Alan C.; Fekner, Tomasz; Spey, Sharon E.; Adams, Harry
Journal of Organic Chemistry, 1999 , vol. 64, # 26 p. 9430 - 9443
