4-(3-溴-苯基)-哌嗪-1-羧酸叔丁酯合成路线 （共 7 条）
反应条件
triethylamine in dichloromethane T=0 - 20°C; 3 h;
参考文献
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Patent: US2009/163508 A1, 2009 ;
Location in patent: Page/Page column 26 ;
US 20090163508 A1
反应条件
tris-(dibenzylideneacetone)dipalladium(0); caesium carbonate; 9,9-dimethyl-4,5-bis(diphenyl-phosphino)xanthene in 1,4-dioxane T=85°C; 16 h; Inert atmosphere;
参考文献
Almirall, S.A.; Vidal Juan, Bernat; Fernandez Collado, Juan Carlos; Erra Sola, Montserrat; Aguilar Izquierdo, Nuria; Mir Cepeda, Marta; Carranco Moruno, Inés
Patent: EP2489663 A1, 2012 ;
Location in patent: Paragraph 0108; 0109 ;
EP 2489663 A1
反应条件
tris-(dibenzylideneacetone)dipalladium(0); potassium tert-butylate; 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl in toluene T=100°C;
参考文献
Castillo, Marcos; Forns, Pilar; Erra, Montse; Mir, Marta; Lopez, Manel; Maldonado, Monica; Orellana, Adelina; Carreno, Cristina; Ramis, Isabel; Miralpeix, Montserrat; Vidal, Bernat
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 17 p. 5419 - 5423
反应条件
nitrogen; potassium acetate in P2O5; 2,4-dimethylbutane; ethyl acetate
参考文献
ASTRAZENECA AB
Patent: US2009/118305 A1, 2009 ;
US 20090118305 A1
反应条件
1,1'-bis-(diphenylphosphino)ferrocene; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate T=80°C;
参考文献
Castillo, Marcos; Forns, Pilar; Erra, Montse; Mir, Marta; Lopez, Manel; Maldonado, Monica; Orellana, Adelina; Carreno, Cristina; Ramis, Isabel; Miralpeix, Montserrat; Vidal, Bernat
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 17 p. 5419 - 5423
反应条件
tetrakis(triphenylphosphine) palladium(0) in N,N-dimethyl-formamide
T=80°C; 12 h;
参考文献
Takeda Pharmaceutical Company Limited
Patent: EP1953148 A1, 2008 ;
Location in patent: Page/Page column 162-163 ;
EP 1953148 A1
反应条件
1: tert-butyl 4-(3-bromophenyl)piperazine-1-carboxylate With n-butyllithium in tetrahydrofuran
T=-70°C; 0.5 h; Inert atmosphere;
2: tri-isopropoxy-borane in tetrahydrofuran
T=-70 - 0°C; Inert atmosphere;
3: With phosphoric acid; ammonium chloride in tetrahydrofuran; water
0.5 h;
参考文献
ARDELYX, INC.; CHARMOT, Dominique; JACOBS, Jeffrey, W.; LEADBETTER, Michael, Robert; NAVRE, Marc; CARRERAS, Chris; BELL, Noah
Patent: WO2010/78449 A2, 2010 ;
Location in patent: Page/Page column 234-235 ;
WO 2010/078449 A2
