1-Boc-4-(4-氰基苯基)哌嗪合成路线 （共 9 条）
反应条件
sodium hydroxide in 1,4-dioxane; water T=20°C; 2 h;
参考文献
Laboratorios Almirall, S.A.
Patent: EP2202232 A1, 2010 ;
Location in patent: Page/Page column 34 ;
反应条件
sodium t-butanolate; tris(dibenzylideneacetone)dipalladium (0); P(i-BuNCH2CH2)3N in toluene T=100°C; Buchwald-Hartwig amination; 24 h;
参考文献
Urgaonkar, Sameer; Verkade, John G.
Journal of Organic Chemistry, 2004 , vol. 69, # 26 p. 9135 - 9142
反应条件
potassium carbonate in dimethyl sulfoxide T=90°C; 8 h;
参考文献
Tangallapally, Rajendra P.; Lee, Robin E.B.; Lenaerts, Anne J.M.; Lee, Richard E.
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2584 - 2589
反应条件
triethylamine in anhydrous xylene; dichloromethane
反应条件
potassium phosphate; Pd0(tris(tert-butyl)phosphine)2 in N,N-dimethyl acetamide T=100°C;
参考文献
Tetrahedron Letters, , vol. 46, # 15 p. 2571 - 2575
反应条件
diisobutylaluminium hydride in hexane; toluene T=50°C; 1.5 h;
参考文献
Schering Corporation
Patent: US2005/239795 A1, 2005 ;
Location in patent: Page/Page column 13 ;
US 20050239795 A1
反应条件
lithium hydroxide; hydrogen; palladium on activated charcoal; nickel in ethyl acetate
参考文献
Tangallapally, Rajendra P.; Lee, Robin E.B.; Lenaerts, Anne J.M.; Lee, Richard E.
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2584 - 2589
反应条件
hydrogenchloride; acetic acid in water T=20°C; 2 h;
参考文献
Berrade, Luis; Aisa, Barbara; Ramirez, Maria J.; Galiano, Silvia; Guccione, Salvatore; Moltzau, Lise Roman; Levy, Finn Olav; Nicoletti, Ferdinando; Battaglia, Giuseppe; Molinaro, Gemma; Aldana, Ignacio; Monge, Antonio; Perez-Silanes, Silvia
Journal of Medicinal Chemistry, 2011 , vol. 54, # 8 p. 3086 - 3090
反应条件
1: H2; LiOH / Raney-Ni; Pd/C / ethyl acetate
2: Et3N / CH2Cl2 / 6 h / 20 °C
3: aq. HCl / tetrahydrofuran / 1 h / 0 - 20 °C
View Scheme
参考文献
Tangallapally, Rajendra P.; Lee, Robin E.B.; Lenaerts, Anne J.M.; Lee, Richard E.
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2584 - 2589
