2-(2,6-二氯-5-氟烟酰基)-3-((2,4-二氟苯基)氨基)丙烯酸乙酯合成路线 （共 11 条）
反应条件
acetic anhydride 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h; Yield given. Multistep reaction;
参考文献
Vymed Corporation; SHETTY, B. Vithal
Patent: US2014/73631 A1, 2014 ;
Location in patent: Paragraph 0128; 0131; 0132 ;
反应条件
1: 1.) n-BuLi, biquinoline / 1.) THF, hexane, from -30 deg C to -5 deg C, 2.) THF, hexane, RT, 1 h 2: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h View Scheme
参考文献
Vymed Corporation; SHETTY, B. Vithal
Patent: US2014/73631 A1, 2014 ;
反应条件
1: thionyl chloride / 2 h / 80 °C 2: 1.) n-BuLi, biquinoline / 1.) THF, hexane, from -30 deg C to -5 deg C, 2.) THF, hexane, RT, 1 h 3: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h View Scheme
参考文献
Vymed Corporation; SHETTY, B. Vithal
Patent: US2014/73631 A1, 2014 ;
反应条件
1: Ac2O / 15 h / 130 °C 2: ethanol / 1 h / Ambient temperature View Scheme
参考文献
Bouzard, D.; Cesare, P. Di; Essiz, M.; Jacquet, J. P.; Ledoussal, B.; et al.
Journal of Medicinal Chemistry, 1992 , vol. 35, # 3 p. 518 - 525
反应条件
1: 73.2 percent / trifluoroacetic acid, 7.5 N aq. HCl / 24 h / Heating 2: thionyl chloride / 2 h / 80 °C 3: 1.) n-BuLi, biquinoline / 1.) THF, hexane, from -30 deg C to -5 deg C, 2.) THF, hexane, RT, 1 h 4: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h View Scheme
参考文献
Vymed Corporation; SHETTY, B. Vithal
Patent: US2014/73631 A1, 2014 ;
反应条件
in ethanol 1 h; Ambient temperature;
参考文献
Bouzard, D.; Cesare, P. Di; Essiz, M.; Jacquet, J. P.; Ledoussal, B.; et al.
Journal of Medicinal Chemistry, 1992 , vol. 35, # 3 p. 518 - 525
反应条件
1: sodium hydride / tetrahydrofuran / 1.5 h / |Inert atmosphere; |Reflux 2: acetic acid; hydrogenchloride / 7.5 h / |Reflux View Scheme
反应条件
1: 86.5 percent / NaH / tetrahydrofuran / 1 h / Heating 2: 85.7 percent / pyridine / 3 h / Ambient temperature View Scheme
参考文献
Chu, Daniel T. W.; Fernandes, Prabhavathi B.; Claiborne, Akiyo K.; Gracey, Eugene H.; Pernet, Andre G.
Journal of Medicinal Chemistry, 1986 , vol. 29, # 11 p. 2364 - 2369
反应条件
1: 86.5 percent / NaH / tetrahydrofuran / 1 h / Heating 2: 85.3 percent / pyridine / 3 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 29, # 11 p. 2364 - 2369
反应条件
1: 86.5 percent / NaH / tetrahydrofuran / 1 h / Heating 2: 81.4 percent / pyridine / 3 h / Ambient temperature View Scheme
参考文献
Chu, Daniel T. W.; Fernandes, Prabhavathi B.; Claiborne, Akiyo K.; Gracey, Eugene H.; Pernet, Andre G.
Journal of Medicinal Chemistry, 1986 , vol. 29, # 11 p. 2364 - 2369
