反应条件
1.1: acetic acid; sodium tris(acetoxy)borohydride / toluene / 16 h / 5 - 20 °C / Molecular sieve
2.1: lithium aluminium tetrahydride / tetrahydrofuran / 2.25 h / 0 - 20 °C
2.2: 16 h / 0 °C
3.1: triethylamine / tetrahydrofuran / 1 h / 0 - 20 °C
4.1: caesium carbonate / tetrahydrofuran / 18 h / 60 °C
5.1: hydrogen / 20 palladium hydroxide on carbon / ethanol / 48 h / 50 °C / 3102.97 Torr
View Scheme
参考文献
JANSSEN PHARMACEUTICA NV; BRANSTETTER, Bryan, James; LETAVIC, Michael, A.; LY, Kiev, S.; RUDOLPH, Dale, A.; SAVALL, Brad, M.; SHAH, Chandravadan, R.; SHIREMAN, Brock, T.
Patent: WO2011/50202 A1, 2011 ;
WO 2011/050202 A1