4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇合成路线 （共 30 条）
反应条件
1: 86.7 percent / piperidine, AcOH / benzene / Heating 2: 1.) HMPA, 2.) DDQ / 1.) 100 deg C, 22 h, 2.) benzene, 30 min 3: 95.7 percent / m-CPBA / CHCl3 / Ambient temperature 4: 46.9 g / ethanol / 1 h / Ambient temperature 5: 1.) NaH / 1.) DMF, 30 min, 2.) DMF, RT, 2 h 6: 277 mg / DIBAL-H / toluene / 1 h / -74 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 5, # 2 p. 437 - 444
反应条件
1: 1.) HMPA, 2.) DDQ / 1.) 100 deg C, 22 h, 2.) benzene, 30 min 2: 95.7 percent / m-CPBA / CHCl3 / Ambient temperature 3: 46.9 g / ethanol / 1 h / Ambient temperature 4: 1.) NaH / 1.) DMF, 30 min, 2.) DMF, RT, 2 h 5: 277 mg / DIBAL-H / toluene / 1 h / -74 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 5, # 2 p. 437 - 444
反应条件
1: 1.) NaH / 1.) DMF, 30 min, 2.) DMF, RT, 2 h 2: 277 mg / DIBAL-H / toluene / 1 h / -74 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 5, # 2 p. 437 - 444
反应条件
1: 95.7 percent / m-CPBA / CHCl3 / Ambient temperature 2: 46.9 g / ethanol / 1 h / Ambient temperature 3: 1.) NaH / 1.) DMF, 30 min, 2.) DMF, RT, 2 h 4: 277 mg / DIBAL-H / toluene / 1 h / -74 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 5, # 2 p. 437 - 444
反应条件
1: 46.9 g / ethanol / 1 h / Ambient temperature 2: 1.) NaH / 1.) DMF, 30 min, 2.) DMF, RT, 2 h 3: 277 mg / DIBAL-H / toluene / 1 h / -74 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 5, # 2 p. 437 - 444
反应条件
1: potassium tert-butylate / tert-butyl alcohol / 24 h / 70 °C 2: triethylamine / dichloromethane / 8 h / -5 °C / Inert atmosphere 3: N-bromosuccinmide / acetonitrile / 16 h / 20 °C / Inert atmosphere; UV-irradiation 4: sodium hydrogencarbonate; dimethyl sulfoxide; sodium iodide / 71 h / 20 °C / Inert atmosphere View Scheme
参考文献
Tetrahedron, , vol. 68, # 9 p. 2155 - 2160
反应条件
1: potassium carbonate / acetone / 48 h / 20 °C / Inert atmosphere 2: potassium tert-butylate / tert-butyl alcohol / 24 h / 70 °C 3: triethylamine / dichloromethane / 8 h / -5 °C / Inert atmosphere 4: N-bromosuccinmide / acetonitrile / 16 h / 20 °C / Inert atmosphere; UV-irradiation 5: sodium hydrogencarbonate; dimethyl sulfoxide; sodium iodide / 71 h / 20 °C / Inert atmosphere View Scheme
参考文献
Tetrahedron, , vol. 68, # 9 p. 2155 - 2160
反应条件
1: N-bromosuccinmide / acetonitrile / 16 h / 20 °C / Inert atmosphere; UV-irradiation 2: sodium hydrogencarbonate; dimethyl sulfoxide; sodium iodide / 71 h / 20 °C / Inert atmosphere View Scheme
参考文献
Tetrahedron, , vol. 68, # 9 p. 2155 - 2160
反应条件
1: triethylamine / dichloromethane / 8 h / -5 °C / Inert atmosphere 2: N-bromosuccinmide / acetonitrile / 16 h / 20 °C / Inert atmosphere; UV-irradiation 3: sodium hydrogencarbonate; dimethyl sulfoxide; sodium iodide / 71 h / 20 °C / Inert atmosphere View Scheme
参考文献
Tetrahedron, , vol. 68, # 9 p. 2155 - 2160
反应条件
1: triethylamine; methanesulfonyl chloride / dichloromethane / 5 h / 0 - 25 °C 2: hydrogen bromide / water / 15 h / 80 °C 3: toluene / 3 h / 0 - 20 °C 4: potassium carbonate / N,N-dimethyl-formamide / 6 h / 70 - 75 °C 5: sulfuric acid / acetonitrile / 3 h / 50 - 60 °C View Scheme
参考文献
YUHAN CORPORATION; JU, Hyun; JOUNG, Sang-Sun; YI, Hyun-Jik; KHOO, Ja-Heouk; LIM, Jong-Chul; KIM, Jae-Gyu
Patent: WO2012/2741 A2, 2012 ;
WO 2012/002741 A2
