4-氨基-1-[(6R,7R,9R)-4-氨基-6-(叔丁基-二甲基硅烷基)氧基-9-[(叔丁基-二甲基硅烷基)氧基甲基]-2,2-二氧代-1,8-二氧杂-2-硫杂螺[4.4]壬-3-烯-7-基]嘧啶-2-酮合成路线 （共 4 条）
反应条件
1: NaHCO3 / H2O; diethyl ether / 4 h / Ambient temperature 2: pyridine / 16 h / 8 - 10 °C 3: aq. TFA / 4 h / Ambient temperature 4: pyridine / Ambient temperature 5: 1.) hexamethyldisilazane, ammonium sulfate, 2.) trimethylsilyl triflate / 1.) reflux, 2.) MeCN, reflux, 5 h 6: Cs2CO3 / acetonitrile / 6 h / Ambient temperature 7: NH3 / methanol / Ambient temperature 8: 4-(dimethylamino)pyridine / acetonitrile / 48 h / Ambient temperature 9: 1.) 1,2,4-triazole, POCl3, pyridine, 2.) aq. NH3 / 1.) RT, 4 h, 2.) RT, 30 min View Scheme
参考文献
Perez-Perez; San-Felix; Balzarini; De Clercq; Camarasa
Journal of Medicinal Chemistry, 1992 , vol. 35, # 16 p. 2988 - 2995
反应条件
1: pyridine / 16 h / 8 - 10 °C 2: aq. TFA / 4 h / Ambient temperature 3: pyridine / Ambient temperature 4: 1.) hexamethyldisilazane, ammonium sulfate, 2.) trimethylsilyl triflate / 1.) reflux, 2.) MeCN, reflux, 5 h 5: Cs2CO3 / acetonitrile / 6 h / Ambient temperature 6: NH3 / methanol / Ambient temperature 7: 4-(dimethylamino)pyridine / acetonitrile / 48 h / Ambient temperature 8: 1.) 1,2,4-triazole, POCl3, pyridine, 2.) aq. NH3 / 1.) RT, 4 h, 2.) RT, 30 min View Scheme
参考文献
Perez-Perez; San-Felix; Balzarini; De Clercq; Camarasa
Journal of Medicinal Chemistry, 1992 , vol. 35, # 16 p. 2988 - 2995
反应条件
1: 4-(dimethylamino)pyridine / acetonitrile / 48 h / Ambient temperature 2: 1.) 1,2,4-triazole, POCl3, pyridine, 2.) aq. NH3 / 1.) RT, 4 h, 2.) RT, 30 min View Scheme
参考文献
Perez-Perez; San-Felix; Balzarini; De Clercq; Camarasa
Journal of Medicinal Chemistry, 1992 , vol. 35, # 16 p. 2988 - 2995
反应条件
pyridine; 1H-1,2,4-triazol; ammonium hydroxide; trichlorophosphate 1.) RT, 4 h, 2.) RT, 30 min; Yield given. Multistep reaction;
参考文献
Perez-Perez; San-Felix; Balzarini; De Clercq; Camarasa
Journal of Medicinal Chemistry, 1992 , vol. 35, # 16 p. 2988 - 2995
