二乙基[[(3-氯-4-氟苯基)氨基]亚甲基]丙二酸酯合成路线 （共 12 条）
反应条件
1: diphenyl ether / 1 h / Heating 2: 90 percent / K2CO3 / dimethylformamide / 10 h / 80 - 90 °C 3: 90 percent / 2N NaOH / 2 h / Heating 4: 66 percent / 5 h / 130 - 140 °C 5: 85 percent / 87percent HCOOH / Heating View Scheme
参考文献
Koga, Hiroshi; Itoh, Akira; Murayama, Satoshi; Suzue, Seigo; Irikura, Tsutomu
Journal of Medicinal Chemistry, 1980 , vol. 23, # 12 p. 1358 - 1363
反应条件
1: diphenyl ether / 1 h / Heating 2: 90 percent / K2CO3 / dimethylformamide / 10 h / 80 - 90 °C 3: 90 percent / 2N NaOH / 2 h / Heating 4: 66 percent / 5 h / 130 - 140 °C View Scheme
参考文献
Koga, Hiroshi; Itoh, Akira; Murayama, Satoshi; Suzue, Seigo; Irikura, Tsutomu
Journal of Medicinal Chemistry, 1980 , vol. 23, # 12 p. 1358 - 1363
反应条件
1: diphenyl ether / 1 h / Heating 2: 90 percent / K2CO3 / dimethylformamide / 10 h / 80 - 90 °C 3: 90 percent / 2N NaOH / 2 h / Heating 4: 32 percent / 5 h / 130 - 140 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 23, # 12 p. 1358 - 1363
反应条件
1: diphenyl ether / 1 h / Heating 2: 90 percent / K2CO3 / dimethylformamide / 10 h / 80 - 90 °C 3: 90 percent / 2N NaOH / 2 h / Heating View Scheme
参考文献
Koga, Hiroshi; Itoh, Akira; Murayama, Satoshi; Suzue, Seigo; Irikura, Tsutomu
Journal of Medicinal Chemistry, 1980 , vol. 23, # 12 p. 1358 - 1363
反应条件
1: diphenyl ether / 1.25 h / 250 °C 2: NaH / dimethylformamide / 5 h / Heating 3: aq. NaOH / 0.5 h / Heating 4: dimethylformamide / 8 h / 140 °C View Scheme
参考文献
Shindikar, Anand V.; Viswanathan
Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 7 p. 1803 - 1806
参考文献
CENTRO MARGA PARA LA INVESTIGACION S.A.
Patent: EP376870 A1, 1990 ;
参考文献
Laboratorie Roger Bellon; Dainippon Pharmaceutical
Patent: US4292317 A1, 1981 ;
US 4292317 A
反应条件
1: Dowtherm A / 1 h / 250 °C
2: potassium carbonate / 1.5 h / 190 °C
View Scheme
参考文献
Koga, Hiroshi; Itoh, Akira; Murayama, Satoshi; Suzue, Seigo; Irikura, Tsutomu
Journal of Medicinal Chemistry, 1980 , vol. 23, # 12 p. 1358 - 1363
反应条件
1: diethyl (4-fluoro-3-chloroanilino)methylenemalonate in diphenylether
Gould-Jacobs reaction; Reflux;
2: With sodium hydroxide in dimethyl sulfoxide
T=20°C; 0.5 h;
3: ethyl iodide in dimethyl sulfoxide
T=20°C; 72 h;
参考文献
Niedermeier, Sabine; Singethan, Katrin; Rohrer, Sebastian G.; Matz, Magnus; Kossner, Markus; Diederich, Sandra; Maisner, Andrea; Schmitz, Jens; Hiltensperger, Georg; Baumann, Knut; Holzgrabe, Ulrike; Schneider-Schaulies, Jurgen
Journal of Medicinal Chemistry, 2009 , vol. 52, # 14 p. 4257 - 4265
反应条件
polyphosphoric acid ethyl ester; potassium carbonate
1.) 100-110 deg C, 3 h, 2.) 190 deg C, 1.5 h; Multistep reaction;
参考文献
Podanyi, Benjamin; Kereszturi, Geza; Vasvari-Debreczy, Lelle; Chinoin, Istvan Hermecz; Toth, Gabor
Magnetic Resonance in Chemistry, 1996 , vol. 34, # 11 p. 972 - 978
