1-萘-2-基-哌嗪盐酸盐合成路线 (共 8 条)
反应条件
1: With Amberlyst(R) 15 in dichloromethane
T=20°C;
2: With ammonium hydroxide in methanol
T=20°C; 1.5 h;
参考文献
Duncton, Matthew A. J.; Roffey, Jonathan R. A.; Hamlyn, Richard J.; Adams, David R.
Tetrahedron Letters, 2006 , vol. 47, # 15 p. 2549 - 2552
反应条件
phosphorus pentoxide; triethyl amine hydrochloride; bis-(2-hydroxy-ethyl)-amine
T=240°C; 0.5 h;
参考文献
NEUROGEN CORPORATION; SCHERING CORPORATION
Patent: EP1025097 B1, 2005 ;
Location in patent: Page/Page column 16 ;
反应条件
potassium carbonate in diethylene glycol dimethyl ether
48 h; Heating;
参考文献
Glennon, Richard A.; Slusher, R. M.; Lyon, Robert A.; Titeler, Milt; McKenney, J. D.
Journal of Medicinal Chemistry, 1986 , vol. 29, # 11 p. 2375 - 2380
反应条件
bis (triortho-tolylphosphine)palladium(II) chloride; sodium t-butanolate in diethylene glycol dimethyl ether
T=170°C; 48 h; Inert atmosphere;
参考文献
Ghosh, Balaram; Antonio, Tamara; Zhen, Juan; Kharkar, Prashant; Reith, Maarten E. A.; Dutta, Aloke K.
Journal of Medicinal Chemistry, 2010 , vol. 53, # 3 p. 1023 - 1037
反应条件
in various solvent(s)
T=150°C;
参考文献
Liu, Kevin G.; Robichaud, Albert J.
Tetrahedron Letters, 2005 , vol. 46, # 46 p. 7921 - 7922
参考文献
Neurogen Corporation
Patent: US6040448 A1, 2000 ;
US 6040448 A
反应条件
1.1: tri-tert-butylphosphine; palladium(II) acetate; sodium tert-butoxide / xylene / 50 °C
1.2: 100 percent / macroporous polymer-supported isocyanate / xylene / 24 h / 50 °C
2.1: Amberlyst(R) 15 / CH2Cl2 / 20 °C
2.2: 65 percent / aq. NH3 / methanol / 1.5 h / 20 °C
View Scheme
参考文献
Duncton, Matthew A. J.; Roffey, Jonathan R. A.; Hamlyn, Richard J.; Adams, David R.
Tetrahedron Letters, 2006 , vol. 47, # 15 p. 2549 - 2552
反应条件
sodium hydrogencarbonate
参考文献
Prelog; Blazek
Collection of Czechoslovak Chemical Communications, 1934 , vol. 6, p. 211,218