[4-(1H-吡唑-1-基)苯基]乙酸合成路线 （共 4 条）
反应条件
1: With lithium hydroxide in tetrahydrofuran; water
T=20°C;
2: With hydrogenchloride in water
pH=~ 3;
参考文献
ACADIA PHARMACEUTICALS INC.
Patent: WO2004/808 A2, 2003 ;
Location in patent: Page 87 ;
WO 2004/000808 A2
反应条件
1: 89 percent / NaBH4, CaCl2 / tetrahydrofuran / Ambient temperature
2: 95 percent / SOCl2 / 1.) RT, 30 min, 2.) reflux, 1.5 h
3: 68 percent / acetonitrile / 3 h / Ambient temperature
4: 93 percent / aq. HCl / 48 h / Heating
View Scheme
参考文献
Artico; Silvestri; Stefancich; Avigliano; Di Giulio; Maccarrone; Agostinelli; Mondovi; Morpurgo
European Journal of Medicinal Chemistry, 1992 , vol. 27, # 3 p. 219 - 228
反应条件
1: 74 percent / NaH / dimethylsulfoxide / 18 h / 100 °C
2: 89 percent / NaBH4, CaCl2 / tetrahydrofuran / Ambient temperature
3: 95 percent / SOCl2 / 1.) RT, 30 min, 2.) reflux, 1.5 h
4: 68 percent / acetonitrile / 3 h / Ambient temperature
5: 93 percent / aq. HCl / 48 h / Heating
View Scheme
参考文献
Artico; Silvestri; Stefancich; Avigliano; Di Giulio; Maccarrone; Agostinelli; Mondovi; Morpurgo
European Journal of Medicinal Chemistry, 1992 , vol. 27, # 3 p. 219 - 228
反应条件
1: 95 percent / SOCl2 / 1.) RT, 30 min, 2.) reflux, 1.5 h
2: 68 percent / acetonitrile / 3 h / Ambient temperature
3: 93 percent / aq. HCl / 48 h / Heating
View Scheme
参考文献
Artico; Silvestri; Stefancich; Avigliano; Di Giulio; Maccarrone; Agostinelli; Mondovi; Morpurgo
European Journal of Medicinal Chemistry, 1992 , vol. 27, # 3 p. 219 - 228
