5-氯-1-(4-氟苯基)-3-(1,2,3,6-四氢吡啶-4-基)-1H-吲哚合成路线 (共 10 条)
反应条件
acetic acid; trifluoroacetic acid 0.5 h; Heating;
参考文献
H. Lundbeck A/S
Patent: EP1260511 A1, 2002 ;
Location in patent: Example 5 ;
反应条件
1: NaBH4 / ethanol; various solvent(s) / 0.5 h / 45 - 55 °C 2: TFA / CH2Cl2 / 1 h / Heating 3: TFA, AcOH / 0.5 h / Heating View Scheme
参考文献
Perregaard; Arnt; Bogeso; Hyttel; Sanchez
Journal of Medicinal Chemistry, 1992 , vol. 35, # 6 p. 1092 - 1101
反应条件
1: TFA / CH2Cl2 / 1 h / Heating 2: TFA, AcOH / 0.5 h / Heating View Scheme
参考文献
Perregaard; Arnt; Bogeso; Hyttel; Sanchez
Journal of Medicinal Chemistry, 1992 , vol. 35, # 6 p. 1092 - 1101
反应条件
1: MgCl2*6H2O, N-methyl-2-pyrrolidone (NMP) / 1 h / 150 °C 2: NaBH4 / ethanol; various solvent(s) / 0.5 h / 45 - 55 °C 3: TFA / CH2Cl2 / 1 h / Heating 4: TFA, AcOH / 0.5 h / Heating View Scheme
参考文献
Perregaard; Arnt; Bogeso; Hyttel; Sanchez
Journal of Medicinal Chemistry, 1992 , vol. 35, # 6 p. 1092 - 1101
反应条件
hydrogenchloride in water; acetic acid T=60 - 95°C; 1.5 h; Heating / refluxIndustry scale;
参考文献
H. Lundbeck A/S
Patent: US6335463 B1, 2002 ;
Location in patent: Page column 7 ;
反应条件
1-(2-chloroethyl)imidazolidin-2-one; sodium carbonate in isobutyl methylketone T=90 - 95°C;
参考文献
H. Lundbeck A/S
Patent: EP1260511 A1, 2002 ;
Location in patent: Example 6 ;
反应条件
sodium carbonate in isobutyl methylketone T=90 - 95°C; Industry scale;
参考文献
H. Lundbeck A/S
Patent: US6335463 B1, 2002 ;
Location in patent: Page column 7 ;
反应条件
potassium carbonate; potassium iodide in various solvent(s) 16 h; Heating;
参考文献
Perregaard; Arnt; Bogeso; Hyttel; Sanchez
Journal of Medicinal Chemistry, 1992 , vol. 35, # 6 p. 1092 - 1101
反应条件
1: H2, AcOH / PtO2 / ethanol / 16 h / 1900 - 2280 Torr 2: 87 percent / K2CO3, KI / various solvent(s) / 16 h / Heating View Scheme
参考文献
Perregaard; Arnt; Bogeso; Hyttel; Sanchez
Journal of Medicinal Chemistry, 1992 , vol. 35, # 6 p. 1092 - 1101
反应条件
hydrogen; acetic acid; platinum(IV) oxide in ethanol P=1900 - 2280 Torr; 16 h;
参考文献
Perregaard; Arnt; Bogeso; Hyttel; Sanchez
Journal of Medicinal Chemistry, 1992 , vol. 35, # 6 p. 1092 - 1101