1-(2,3-二氯苯基)哌嗪合成路线 （共 13 条）
反应条件
phosphorus pentoxide; triethyl amine hydrochloride T=220°C; 4 h;
参考文献
Robarge; Husbands; Kieltyka; Brodbeck; Thurkauf; Newman
Journal of Medicinal Chemistry, 2001 , vol. 44, # 19 p. 3175 - 3186
反应条件
2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl; 1,8-diazabicyclo[5.4.0]undec-7-ene; sodium t-butanolate; tris(dibenzylideneacetone)dipalladium (0) in toluene T=60 - 70°C; Buchwald amination;
参考文献
Torisawa, Yasuhiro; Nishi, Takao; Minamikawa, Jun-Ichi
Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 12 p. 4023 - 4027
反应条件
tris(dibenzylideneacetone)dipalladium (0); (R)-1,1'-bis(diphenylphosphino)-2,2'-binapthyl; sodium t-butanolate in toluene 18 h; Heating;
参考文献
Morita, Seiji; Kitano, Kazuyoshi; Matsubara, Jun; Ohtani, Tadaaki; Kawano, Yoshikazu; Otsubo, Kenji; Uchida, Minoru
Tetrahedron, 1998 , vol. 54, # 19 p. 4811 - 4818
反应条件
1: dimethylformamide / 5 h / 100 °C 2: LiAlH4 / tetrahydrofuran / 5 h View Scheme
参考文献
Dutta, Aloke K.; Venkataraman, Sylesh K.; Fei, Xiang-Shu; Kolhatkar, Rohit; Zhang, Shijun; Reith, Maarten E.A.
Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 16 p. 4361 - 4373
反应条件
1: 7-(4-chlorobutoxy)-3,4-dihydroquinolin-2(1H)-one With sodium iodide in N,N-dimethyl-formamide T=70 - 80°C; 1 h; 2: 1-(2,3-dichloro-phenyl)-piperazine With potassium carbonate in N,N-dimethyl-formamide T=70 - 80°C; 4 h;
参考文献
UNICHEM LABORATORIES LIMITED
Patent: WO2007/94009 A1, 2007 ;
Location in patent: Page/Page column 7-8 ;
反应条件
hydrogen; [rhodium(I)(carbonyl)2(acetylacetonate)]; 6,6'-[[3,3',5,5'-tetrakis(1,1-dimethylethyl)-[1,1'-biphenyl]-2,2'-diyl]bis(oxy)]bis-dibenzo [d,f][1,3,2]-dioxaphosphepine in tetrahydrofuran T=75°C; P=20702.1 Torr; 16 h;
参考文献
UNION CARBIDE CHEMICALS and PLASTICS TECHNOLOGY CORPORATION
Patent: WO2005/77884 A2, 2005 ;
Location in patent: Page/Page column 19-20 ;
反应条件
triethylamine in acetonitrile T=30 - 81°C; 4 - 5 h; Product distribution / selectivity;
参考文献
CADILA PHARMACEUTICALS LIMITED
Patent: WO2008/1188 A2, 2008 ;
Location in patent: Page/Page column 9-10 ;
反应条件
[rhodium(I)(carbonyl)2(acetylacetonate)]; 6,6'-[[3,3',5,5'-tetrakis(1,1-dimethylethyl)-[1,1'-biphenyl]-2,2'-diyl]bis(oxy)]bis-dibenzo [d,f][1,3,2]-dioxaphosphepine; hydrogen in tetrahydrofuran T=75°C; P=20685.9 Torr; 16 h;
参考文献
Briggs, John R.; Klosin, Jerzy; Whiteker, Gregory T.
Organic Letters, 2005 , vol. 7, # 22 p. 4795 - 4798
反应条件
1: 7-(4-bromobutoxy)-3,4-dihydro-quinolin-2(1H)-one With sodium iodide in methanol T=25 - 35°C; 0.5 h; 2: 1-(2,3-dichloro-phenyl)-piperazine With triethylamine in acetonitrile T=25 - 35°C; 15.5 h; Heating / reflux; Product distribution / selectivity;
参考文献
KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO
Patent: WO2008/34628 A1, 2008 ;
Location in patent: Page/Page column 14-15 ;
反应条件
triethylamine; sodium iodide in acetonitrile 4 h; Heating;
参考文献
Oshiro, Yasuo; Sato, Seiji; Kurahashi, Nobuyuki; Tanaka, Tatsuyoshi; Kikuchi, Tetsuro; Tottori, Katsura; Uwahodo, Yasufumi; Nishi, Takao
Journal of Medicinal Chemistry, 1998 , vol. 41, # 5 p. 658 - 667
