3-(2-甲氧基-2-氧代乙基)苯硼酸频那醇酯合成路线 （共 7 条）
反应条件
potassium acetate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct in dimethyl sulfoxide
T=80°C; Suzuki reaction; 3 h;
参考文献
Kranich, Remo; Busemann, Anke S.; Bock, Daniel; Schroeter-Maas, Sabine; Beyer, Diana; Heinemann, Bo; Meyer, Michael; Schierhorn, Katrin; Zahlten, Rainer; Wolff, Gerhard; Aydt, Ewald M.
Journal of Medicinal Chemistry, 2007 , vol. 50, # 6 p. 1101 - 1115
反应条件
(1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate in N,N-dimethyl-formamide
T=70 - 90°C; 3 h;
参考文献
Robichaud, Joel; Oballa, Renata; Prasit, Peppi; Falgueyret, Jean-Pierre; Percival, M. David; Wesolowski, Gregg; Rodan, Sevgi B.; Kimmel, Donald; Johnson, Colena; Bryant, Cliff; Venkatraman, Shankar; Setti, Eduardo; Mendonca, Rohan; Palmer, James T.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 17 p. 3709 - 3727
反应条件
1: With hydrogenchloride in diethyl ether
48 h; cooling;
2: With methanol in diethyl ether
T=20°C; 24 h; Further stages.;
参考文献
Morandi, Stefania; Morandi, Federica; Caselli, Emilia; Shoichet, Brian K.; Prati, Fabio
Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 3 p. 1195 - 1205
反应条件
1: thionyl chloride / 2 h / 10 - 20 °C
2: potassium acetate / palladium(II) dichloride bis[bis(diphenylphosphine)ferrocene] / N,N-dimethyl-formamide
View Scheme
参考文献
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Patent: US2011/257172 A1, 2011 ;
反应条件
1: 100 percent / p-TsOH / methanol / 4 h / Heating
2: 82 percent / Et3N / CH2Cl2 / 1 h / 0 °C
3: 90 percent / KOAc; Pd(Cl)2dppf / dimethylformamide / 3 h / 70 - 90 °C
View Scheme
参考文献
Robichaud, Joel; Oballa, Renata; Prasit, Peppi; Falgueyret, Jean-Pierre; Percival, M. David; Wesolowski, Gregg; Rodan, Sevgi B.; Kimmel, Donald; Johnson, Colena; Bryant, Cliff; Venkatraman, Shankar; Setti, Eduardo; Mendonca, Rohan; Palmer, James T.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 17 p. 3709 - 3727
反应条件
1: 82 percent / Et3N / CH2Cl2 / 1 h / 0 °C
2: 90 percent / KOAc; Pd(Cl)2dppf / dimethylformamide / 3 h / 70 - 90 °C
View Scheme
参考文献
Robichaud, Joel; Oballa, Renata; Prasit, Peppi; Falgueyret, Jean-Pierre; Percival, M. David; Wesolowski, Gregg; Rodan, Sevgi B.; Kimmel, Donald; Johnson, Colena; Bryant, Cliff; Venkatraman, Shankar; Setti, Eduardo; Mendonca, Rohan; Palmer, James T.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 17 p. 3709 - 3727
参考文献
Eisai Co., Ltd.
Patent: EP1394147 A1, 2004 ;
Location in patent: Page 143 ;
