1-(4-氯苄基)哌啶-4-胺三氟乙酸酯合成路线 （共 6 条）
反应条件
1: With sodium tetrahydroborate in tetrahydrofuran; methanol
T=15 - 26°C;
2: With sodium hydroxide in tetrahydrofuran; methanol; water
Product distribution / selectivity;
参考文献
ASTRAZENECA AB
Patent: WO2009/35407 A1, 2009 ;
Location in patent: Page/Page column 10; 21 ;
反应条件
1: With trifluoroacetic acid in dichloromethane
2: With sodium hydroxide in dichloromethane
参考文献
Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 7 p. 2917 - 2929
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
lithium aluminium tetrahydride in tetrahydrofuran; diethyl ether
19 h; Heating;
参考文献
Moragues; Prieto; Spickett; Vega; Salazar; Roberts
Farmaco, Edizione Scientifica, 1980 , vol. 35, # 11 p. 951 - 964
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: thionyl chloride / dichloromethane / 0 - 20 °C
2: triethylamine / tetrahydrofuran / Reflux
3: trifluoroacetic acid / dichloromethane
View Scheme
参考文献
Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 7 p. 2917 - 2929
