4-(4-氟苯基)-1-甲基哌啶-4-甲腈合成路线 (共 7 条)
反应条件
sodium hydride in N,N-dimethyl-formamide T=0 - 60°C; 24 h;
参考文献
ASTRAZENECA AB
Patent: WO2004/56771 A1, 2004 ;
Location in patent: Page 12 ;
WO 2004/056771 A1
反应条件
1: 66 percent / NaNH2 / toluene / Heating 2: aq. HCl / 50 °C 3: 0.63 g / NaBH3CN / methanol / 48 h View Scheme
参考文献
Lomenzo, Stacey A.; Izenwasser, Sari; Gerdes, Robert M.; Katz, Jonathan L.; Kopajtic, Theresa; Trudell, Mark L.
Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 23 p. 3273 - 3276
反应条件
1: aq. HCl / 50 °C 2: 0.63 g / NaBH3CN / methanol / 48 h View Scheme
参考文献
Lomenzo, Stacey A.; Izenwasser, Sari; Gerdes, Robert M.; Katz, Jonathan L.; Kopajtic, Theresa; Trudell, Mark L.
Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 23 p. 3273 - 3276
反应条件
sodium cyanoborohydride in methanol 48 h;
参考文献
Lomenzo, Stacey A.; Rhoden, Jill B.; Izenwasser, Sari; Wade, Dean; Kopajtic, Theresa; Katz, Jonathan L.; Trudell, Mark L.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 5 p. 1336 - 1343
反应条件
sodium cyanoborohydride in methanol Reductive amination;
参考文献
Lomenzo, Stacey A.; Izenwasser, Sari; Gerdes, Robert M.; Katz, Jonathan L.; Kopajtic, Theresa; Trudell, Mark L.
Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 23 p. 3273 - 3276
反应条件
1: 4-(4-fluorophenyl)-1-methylpiperidine-4-carbonitrile With 1-chloroethyl chlorocarbonate in 1,2-dichloro-ethane T=85°C; 2: di-tert-butyl dicarbonate With sodium hydroxide in methanol
参考文献
Liu, Jian; Jian, Tianying; Sebhat, Iyassu; Nargund, Ravi
Tetrahedron Letters, 2006 , vol. 47, # 29 p. 5115 - 5117
反应条件
1.1: 1-chloroethylchloroformate / 1,2-dichloro-ethane / 85 °C
1.2: aq. NaOH / methanol
2.1: BH3-THF / 40 °C
View Scheme
参考文献
Liu, Jian; Jian, Tianying; Sebhat, Iyassu; Nargund, Ravi
Tetrahedron Letters, 2006 , vol. 47, # 29 p. 5115 - 5117