1-苄基-4-苯基氨基-4-哌啶羧酸乙酯合成路线 （共 9 条）
反应条件
1: 4-phenylamino-1-benzyl-4-piperidinecarboxylic acid With sodium hydroxide in methanol
0.5 h; Heating / reflux;
2: ethyl bromide in N,N,N',N',N'',N''-hexamethylphosphoric triamide
T=20°C;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2006/105035 A2, 2006 ;
Location in patent: Page/Page column 56-57 ;
WO 2006/105035 A2
反应条件
in toluene
240 h; Heating;
参考文献
Colapret; Diamantidis; Spencer; Spaulding; Rudo
Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 968 - 974
反应条件
1: Na2HPO4 / CH2Cl2 / 18 h / 0 - 20 °C
2: 411.2 mg / HCl / H2O / Ambient temperature; 4-5 h
View Scheme
参考文献
Kiessling, Anthony J.; McClure, Cynthia K.
Synthetic Communications, 1997 , vol. 27, # 5 p. 923 - 937
反应条件
2: H2SO4
3: conc. HCl / Heating
4: 80 percent / toluene / 240 h / Heating
View Scheme
参考文献
Colapret; Diamantidis; Spencer; Spaulding; Rudo
Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 968 - 974
反应条件
1: H2SO4
2: conc. HCl / Heating
3: 80 percent / toluene / 240 h / Heating
View Scheme
参考文献
Colapret; Diamantidis; Spencer; Spaulding; Rudo
Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 968 - 974
反应条件
2: H2SO4
3: conc. HCl / Heating
4: 80 percent / toluene / 240 h / Heating
View Scheme
参考文献
Colapret; Diamantidis; Spencer; Spaulding; Rudo
Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 968 - 974
反应条件
sulfuric acid
1.) 70 deg C; 2.) hexamethylphosphoric triamide, 20 deg C, 24 h; Yield given. Multistep reaction;
参考文献
Parys, Marc Van; Vandewalle, Maurits
Bulletin des Societes Chimiques Belges, 1981 , vol. 90, # 7 p. 749 - 756
反应条件
lithium aluminium tetrahydride in tetrahydrofuran; dichloromethane
Ambient temperature;
参考文献
Colapret; Diamantidis; Spencer; Spaulding; Rudo
Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 968 - 974
反应条件
in isopropyl alcohol; acetonitrile; benzene
参考文献
Janssen Pharmaceutica N.V.
Patent: US4179569 A1, 1979 ;
