4-(1H-苯并咪唑-2-基氨基)-1-哌啶羧酸乙酯合成路线 (共 15 条)
反应条件
potassium carbonate; potassium iodide in N,N-dimethyl-formamide T=70 - 80°C; 20 h;
参考文献
Roman, Gheorghe; Crandall, Ian E.; Szarek, Walter A.
ChemMedChem, 2013 , vol. 8, # 11 p. 1795 - 1804
反应条件
1: 40 percent / sodium carbonate, potassium iodide / dimethylformamide / 70 °C 2: 82 percent / 48 percent hydrobromic acid / 1 h / Heating 3: 48 percent / Na2CO3 / dimethylformamide / 70 °C View Scheme
参考文献
Janssens, Frans; Torremans, Joseph; Janssen, Marcel; Stokbroekx, Raymond A.; Luyckx, Marcel; Janssen, Paul A. J.
Journal of Medicinal Chemistry, 1985 , vol. 28, # 12 p. 1934 - 1943
反应条件
1: 40 percent / sodium carbonate, potassium iodide / dimethylformamide / 70 °C 2: 82 percent / 48 percent hydrobromic acid / 1 h / Heating 3: 46.7 percent / Na2CO3 / dimethylformamide / 20 h / 70 °C 4: 88.5 percent / H2 / 10 percent Pd/C / methanol View Scheme
参考文献
Janssens, Frans; Torremans, Joseph; Janssen, Marcel; Stokbroekx, Raymond A.; Luyckx, Marcel; Janssen, Paul A. J.
Journal of Medicinal Chemistry, 1985 , vol. 28, # 12 p. 1934 - 1943
反应条件
sulfur; mercury(II) oxide in ethanol
2 h; Heating;
参考文献
Janssens; Torremans; Janssen; Stokbroekx; Luyckx
Journal of Medicinal Chemistry, 1985 , vol. 28, # 12 p. 1925 - 1933
参考文献
Ishikawa, Minoru; Kubota, Dai; Yamamoto, Mikio; Kuroda, Chizuko; Iguchi, Maki; Koyanagi, Akihiro; Murakami, Shoichi; Ajito, Keiichi
Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 7 p. 2109 - 2130
参考文献
Janssen Pharmaceutica N.V.
Patent: US4219559 A1, 1980 ;
反应条件
1: 1.) sodium hydroxide, 2.) ethyl chloroformate / 1.) water, 10 deg C, 30 min, 2.) water, 60 deg C, 2 h
2: 100 percent / ethanol / Ambient temperature
3: 55.5 percent / yellow HgO, sulfur / ethanol / 2 h / Heating
View Scheme
参考文献
Janssens; Torremans; Janssen; Stokbroekx; Luyckx
Journal of Medicinal Chemistry, 1985 , vol. 28, # 12 p. 1925 - 1933
反应条件
1: 100 percent / ethanol / Ambient temperature
2: 55.5 percent / yellow HgO, sulfur / ethanol / 2 h / Heating
View Scheme
参考文献
Janssens; Torremans; Janssen; Stokbroekx; Luyckx
Journal of Medicinal Chemistry, 1985 , vol. 28, # 12 p. 1925 - 1933
反应条件
in chloroform; ethyl acetate
参考文献
Meiji Seika Kaisha, Ltd.
Patent: US6420558 B1, 2002 ;
反应条件
tris-(dibenzylideneacetone)dipalladium(0); 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl; sodium t-butanolate in toluene
T=85°C; acidic (aq. HCl) work-up;
参考文献
Hong, Yaping; Senanayake, Chris H.; Xiang, Tingjian; Vandenbossche, Charles P.; Tanoury, Gerald J.; Bakale, Roger P.; Wald, Stephen A.
Tetrahedron Letters, 1998 , vol. 39, # 20 p. 3121 - 3124