5,7-二氯-1-甲基-吡唑并[4,3-d]嘧啶合成路线 （共 5 条）
反应条件
N,N-diethylaniline; trichlorophosphate
T=130°C; 18 h; Inert atmosphere;
参考文献
Lee, Wendy; Ortwine, Daniel F.; Bergeron, Philippe; Lau, Kevin; Lin, Lichuan; Malek, Shiva; Nonomiya, Jim; Pei, Zhonghua; Robarge, Kirk D.; Schmidt, Stephen; Sideris, Steve; Lyssikatos, Joseph P.
Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 18 p. 5097 - 5104
反应条件
1.1: 2 h / 200 °C / Neat (no solvent)
2.1: 1,8-diazabicyclo[5.4.0]undec-7-ene; trichlorophosphate / 8 h / 50 - 80 °C / Inert atmosphere
2.2: pH 7
View Scheme
参考文献
Baraldi, Pier Giovanni; Saponaro, Giulia; Aghazadeh Tabrizi, Mojgan; Baraldi, Stefania; Romagnoli, Romeo; Moorman, Allan R.; Varani, Katia; Borea, Pier Andrea; Preti, Delia
Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 2 p. 1046 - 1059
反应条件
1: acetonitrile / 19 h / 100 °C / Inert atmosphere
2: N,N-diethylaniline; trichlorophosphate / 18 h / 130 °C / Inert atmosphere
View Scheme
参考文献
Genentech, Inc.
Patent: US2011/86840 A1, 2011 ;
反应条件
1.1: palladium 10 on activated carbon; hydrogen / ethanol / 5 h / 20 °C / 2585.81 Torr
2.1: 2 h / 200 °C / Neat (no solvent)
3.1: 1,8-diazabicyclo[5.4.0]undec-7-ene; trichlorophosphate / 8 h / 50 - 80 °C / Inert atmosphere
3.2: pH 7
View Scheme
参考文献
Baraldi, Pier Giovanni; Saponaro, Giulia; Aghazadeh Tabrizi, Mojgan; Baraldi, Stefania; Romagnoli, Romeo; Moorman, Allan R.; Varani, Katia; Borea, Pier Andrea; Preti, Delia
Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 2 p. 1046 - 1059
反应条件
1.1: nitric acid; sulfuric acid / 0 °C / |Inert atmosphere
1.2: 0 - 20 °C
1.3: 3102.97 Torr
2.1: acetonitrile / 19 h / 100 °C / |Inert atmosphere; |Reflux
3.1: trichlorophosphate; N,N-diethylaniline / 18 h / 130 °C / |Inert atmosphere
View Scheme
参考文献
Lee, Wendy; Ortwine, Daniel F.; Bergeron, Philippe; Lau, Kevin; Lin, Lichuan; Malek, Shiva; Nonomiya, Jim; Pei, Zhonghua; Robarge, Kirk D.; Schmidt, Stephen; Sideris, Steve; Lyssikatos, Joseph P.
Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 18 p. 5097 - 5104
