4-氨基-1-苄基哌啶-4-甲腈合成路线 （共 10 条）
反应条件
ammonium chloride in methanol T=25°C; 12 h;
参考文献
Chaturvedula, Prasad V.; Pin, Sokhom; Tholady, George; Conway, Charlie M.; MacOr, John E.; Dubowchik, Gene M.
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 14 p. 4719 - 4722
反应条件
1: With zinc(II) iodide in dichloromethane T=23°C; 16 h; 2: With ammonia in methanol; dichloromethane T=40°C;
参考文献
SCHERING CORPORATION
Patent: EP1032561 B1, 2004 ;
Location in patent: Page 17 ;
EP 1032561 B1
反应条件
ammonium chloride in ethanol; water 48 h; Ambient temperature;
参考文献
Metwally, Kamel A.; Dukat, Malgorzata; Egan, Christina T.; Smith, Carol; DuPre, Ann; Gauthier, Colleen B.; Herrick-Davis, Katharine; Teitler, Milt; Glennon, Richard A.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 25 p. 5084 - 5093
反应条件
1: With ammonium chloride in water 144 h; 2: With potassium carbonate in water T=0°C; pH=11;
参考文献
Cumbre Inc.
Patent: US2005/277633 A1, 2005 ;
Location in patent: Page/Page column 17 ;
US 20050277633 A1
反应条件
sodium hydroxide; lithium aluminum hydride; magnesium sulfate in tetrahydrofuran; methanol; diethyl ether; dichloromethane; water
参考文献
Vertex Pharmaceuticals Incorported
Patent: US2011/98311 A1, 2011 ;
反应条件
ammonium hydroxide; ammonium chloride in water Addition; 0.5 h;
参考文献
Marco, Jose L.; Ingate; Chinchon
Tetrahedron, 1999 , vol. 55, # 24 p. 7625 - 7644
反应条件
1: sodium cyanide; ammonium chloride; ammonia / 2,4-dimethylbutane; water 2: sodium hydroxide; lithium aluminum hydride; magnesium sulfate / tetrahydrofuran; methanol; diethyl ether; dichloromethane; water View Scheme
参考文献
Vertex Pharmaceuticals Incorported
Patent: US2011/98311 A1, 2011 ;
反应条件
1: 75 percent / H2SO4 / 5 h / Ambient temperature 2: 1.) conc. H2SO4, 2.) NaBH4 / 1.) reflux, 20 h, 2.) MeOH, 60 deg C, 1 h View Scheme
参考文献
Metwally, Kamel A.; Dukat, Malgorzata; Egan, Christina T.; Smith, Carol; DuPre, Ann; Gauthier, Colleen B.; Herrick-Davis, Katharine; Teitler, Milt; Glennon, Richard A.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 25 p. 5084 - 5093
反应条件
1: With sulfuric acid in dichloromethane T=0 - 5°C; 2: With sodium hydroxide in water T=10°C; pH=9;
参考文献
JANSSEN PHARMACEUTICA NV; BIGNAN, Gilles C.; CONNOLLY, Peter J.; LU, Tianbao L.; PARKER, Michael H.; LUDOVICI, Donald; MEYER, Christophe; MEERPOEL, Lieven; SMANS, Karine; ROCABOY, Christian
Patent: WO2014/39769 A1, 2014 ;
Location in patent: Page/Page column 287 ;
反应条件
1: 75 percent / H2SO4 / 5 h / Ambient temperature
2: 1.) conc. H2SO4, 2.) NaBH4 / 1.) reflux, 20 h, 2.) MeOH, 60 deg C, 1 h
3: 79 percent / H2, 35 percent HCl in MeOH / 10 percent Pd/C / 8 h / 2068.59 Torr / Ambient temperature
View Scheme
参考文献
Metwally, Kamel A.; Dukat, Malgorzata; Egan, Christina T.; Smith, Carol; DuPre, Ann; Gauthier, Colleen B.; Herrick-Davis, Katharine; Teitler, Milt; Glennon, Richard A.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 25 p. 5084 - 5093
