1-(4-氟苄基)哌啶-4-胺合成路线 (共 6 条)
反应条件
1: With N-ethyl-N,N-diisopropylamine in dichloromethane
T=20°C; 64 h;
2: With trifluoroacetic acid in dichloromethane
T=20°C; 1 h;
3: With ammonia; acetic acid
more than 3 stages;
参考文献
ASTRAZENECA AB
Patent: WO2007/53082 A1, 2007 ;
Location in patent: Page/Page column 52 ;
WO 2007/053082 A1
反应条件
triethylamine in chloroform
参考文献
Nisshin Flour Milling Co., Ltd.
Patent: US5736550 A1, 1998 ;
反应条件
1: With trifluoroacetic acid in dichloromethane
5 h;
2: With sodium hydroxide
Product distribution / selectivity;
参考文献
KHAMRAI, Uttam; Ronsheim, Matthew; Karak, Sumit Kumar
Patent: US2010/152160 A1, 2010 ;
Location in patent: Page/Page column 31 ;
US 20100152160 A1
反应条件
bis-[(trifluoroacetoxy)iodo]benzene in water; acetonitrile
T=65°C; Hoffmann rearrangement;
参考文献
Shum; Peet; Weintraub; Le; Zhao; Barbone; Cashman; Tsay; Dwyer; Loos; Powers; Kropp; Wright; Bitonti; Dumont; Borcherding
Nucleosides, Nucleotides and Nucleic Acids, 2001 , vol. 20, # 4-7 p. 1067 - 1078
反应条件
1: Cs2CO3; KI / various solvent(s) / 5 h / 100 °C
2: PhI(CF3CO2)2 / acetonitrile; H2O / 65 °C
View Scheme
参考文献
Shum; Peet; Weintraub; Le; Zhao; Barbone; Cashman; Tsay; Dwyer; Loos; Powers; Kropp; Wright; Bitonti; Dumont; Borcherding
Nucleosides, Nucleotides and Nucleic Acids, 2001 , vol. 20, # 4-7 p. 1067 - 1078
反应条件
1: triethylamine / dichloromethane / 20 °C / Cooling with ice; Inert atmosphere
2: trifluoroacetic acid / dichloromethane / 20 °C
View Scheme
参考文献
Mao, Yongjun; Lin, Nan; Tian, Wang; Han, Xiaofeng; Han, Xiaobing; Huang, Ziwei; An, Jing
Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1346 - 1359