5-氯-3-碘-1H-吡唑并[3,4-b]吡啶合成路线 (共 3 条)
反应条件
N-iodo-succinimide in 1,2-dichloro-ethane T=20 - 50°C; 64 h;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; CHARIFSON, Paul, S.; CLARK, Michael, P.; BANDARAGE, Upul, K.; DAVIES, Ioana; DUFFY, John, P.; GAO, Huai; FENG, Jun; LIANG, Jianglin; KENNEDY, Joseph, M.; LEDEBOER, Mark, W.; LEDFORD, Brian; MALTAIS, Francois; PEROLA, Emanuele
Patent: WO2012/83117 A1, 2012 ;
Location in patent: Page/Page column 122 ;
反应条件
1.1: N-ethyl-N,N-diisopropylamine; n-butyllithium / tetrahydrofuran / 1.5 h / -78 °C 1.2: 0.03 h 2.1: toluene-4-sulfonic acid / toluene / 3 h / Reflux 3.1: hydrazine; N-ethyl-N,N-diisopropylamine / isopropyl alcohol / 65 °C 4.1: N-iodo-succinimide / 1,2-dichloro-ethane / 64 h / 20 - 50 °C View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; CHARIFSON, Paul, S.; CLARK, Michael, P.; BANDARAGE, Upul, K.; DAVIES, Ioana; DUFFY, John, P.; GAO, Huai; FENG, Jun; LIANG, Jianglin; KENNEDY, Joseph, M.; LEDEBOER, Mark, W.; LEDFORD, Brian; MALTAIS, Francois; PEROLA, Emanuele
Patent: WO2012/83117 A1, 2012 ;
反应条件
1: hydrazine; N-ethyl-N,N-diisopropylamine / isopropyl alcohol / 65 °C 2: N-iodo-succinimide / 1,2-dichloro-ethane / 64 h / 20 - 50 °C View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; CHARIFSON, Paul, S.; CLARK, Michael, P.; BANDARAGE, Upul, K.; DAVIES, Ioana; DUFFY, John, P.; GAO, Huai; FENG, Jun; LIANG, Jianglin; KENNEDY, Joseph, M.; LEDEBOER, Mark, W.; LEDFORD, Brian; MALTAIS, Francois; PEROLA, Emanuele
Patent: WO2012/83117 A1, 2012 ;