1-乙酰基-4-(4-羟基苯基)哌嗪合成路线 （共 13 条）
反应条件
1: With pyridine T=0 - 20°C; 3.08333 h; 2: With methanol; water; potassium carbonate 1.5 h; 3: With hydrogenchloride; water in dichloromethane pH=3;
参考文献
GALAPAGOS N.V.
Patent: WO2008/55959 A1, 2008 ;
Location in patent: Page/Page column 67 ;
WO 2008/055959 A1
反应条件
water; potassium hydrogencarbonate in methanol Ambient temperature;
参考文献
Stefancich; Artico; Ortar; Silvestri; Simonetti; Apuzzo
Archiv der Pharmazie, 1992 , vol. 325, # 11 p. 687 - 694
反应条件
sodium hydroxide; oxalic acid; triphenylphosphine in tetrahydrofuran; diethyl ether; dichloromethane; ethyl acetate
反应条件
anhydrous sodium hydrogen carbonate; acetic anhydride; potassium carbonate in hydrogenchloride; water
反应条件
1: 100 percent / sodium acetate / acetic acid / 0.75 h / Heating 2: 92 percent / KHCO3, H2O / methanol / Ambient temperature View Scheme
参考文献
Archiv der Pharmazie, , vol. 325, # 11 p. 687 - 694
反应条件
1: pyridine / CH2Cl2 2: K2CO3 / methanol / 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 16, # 4 p. 887 - 890
反应条件
1: 100 percent / 48 percent HBr / Heating; overnight 2: 100 percent / sodium acetate / acetic acid / 0.75 h / Heating 3: 92 percent / KHCO3, H2O / methanol / Ambient temperature View Scheme
参考文献
Archiv der Pharmazie, , vol. 325, # 11 p. 687 - 694
反应条件
1: 88 percent / 48percent HBr / 4 h / 140 °C 2: pyridine / 12 h / Ambient temperature 3: NH4OH / methanol / Ambient temperature; 12 + 2 h View Scheme
参考文献
Journal of Heterocyclic Chemistry, , vol. 27, # 7 p. 2063 - 2068
反应条件
sodium hydride 1.) DMSO, RT, 1 h, 2.) DMSO, 80 deg C, 4 h; Yield given. Multistep reaction;
参考文献
Camps, Pelayo; Farres, Xavier; Garcia, Luisa; Ginesta, Joan; Pascual, Jaume; et al.
Tetrahedron: Asymmetry, 1995 , vol. 6, # 6 p. 1283 - 1294
反应条件
sodium hydride in dimethyl sulfoxide T=0 - 80°C;
参考文献
Power, Eoin C.; Ganellin, C. Robin; Benton, David C.H.
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 4 p. 887 - 890
