2,6-二氯-5-氟烟酰乙酸乙酯合成路线 （共 28 条）
反应条件
1: 81 percent / 35percent HCl / 3 h / 135 - 140 °C 2: 81 percent / SOCl2 / 1 h / Heating 3: 1.) Mg, CCl4, EtOH / 1.) Et2O, reflux, 30 min, 2.) 10 min 4: p-toluenesulfonic acid / H2O / 2 h / Heating View Scheme
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 38, # 12 p. 3211 - 3217
反应条件
toluene-4-sulfonic acid 1.) ether, RT, 2 h, 2.) H2O, reflux, 2.5 h; Multistep reaction;
参考文献
Journal of Medicinal Chemistry, , vol. 35, # 3 p. 518 - 525
反应条件
1: in tetrahydrofuran 2: With methylmagnesium bromide in tetrahydrofuran
参考文献
European Journal of Medicinal Chemistry, , vol. 44, # 8 p. 3356 - 3362
反应条件
triethylamine; magnesium chloride 1.) EtOAc, a) 35 deg C, 30 min, b) 35 deg C, 6 h, 2.) 20 to 25 deg C, 12 h; Yield given. Multistep reaction;
参考文献
Synthesis, , # 3 p. 290 - 292
反应条件
1: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h 2: 59.6 percent / NaH / tetrahydrofuran / 1 h / Heating 3: 60 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
1.1: acetic anhydride / 1 h / 130 °C 1.2: 1 h 2.1: sodium hydride / tetrahydrofuran / 1.5 h / |Inert atmosphere; |Reflux 3.1: acetic acid; hydrogenchloride / 7.5 h / |Reflux View Scheme
反应条件
1.1: Ac2O / 1 h / 140 °C 1.2: 90 percent / ethanol / 20 °C 2.1: K2CO3 / dioxane View Scheme
参考文献
Karoli, Tomislav; Mamidyala, Sreeman K.; Zuegg, Johannes; Fry, Scott R.; Tee, Ernest H.L.; Bradford, Tanya A.; Madala, Praveen K.; Huang, Johnny X.; Ramu, Soumya; Butler, Mark S.; Cooper, Matthew A.
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2428 - 2433
反应条件
1: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h 2: 86.5 percent / NaH / tetrahydrofuran / 1 h / Heating 3: 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: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h 2: 59.6 percent / NaH / tetrahydrofuran / 1 h / Heating 3: 88.1 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: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h 2: 86.5 percent / NaH / tetrahydrofuran / 1 h / Heating 3: 85.3 percent / pyridine / 3 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 29, # 11 p. 2364 - 2369
