反应详情

温度

140 °C

A mixture of ((2R)-4-(thiophen-2-ylsulfonyl)-1-(4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl)piperazin-2-yl)methyl methanesulfonate (0.9 g, 1.70 mmol, Intermediate B) in 2 M NH3 in MeOH (10 mL, 20.0 mmol) was heated in an Initiator microwave reactor (Biotage AB, Inc., Uppsala, Sweden) at 140° C. for 30 min. The mixture was concentrated and purified on silica gel [2% MeOH in CH2Cl2 to 2% (2 N NH3-MeOH) in CH2Cl2) to give 2-(4-((2S)-2-(aminomethyl)-4-(2-thiophenylsulfonyl)-1-piperazinyl)phenyl)-1,1,1-trifluoro-2-propanol as a white foam (500 mg).

1. concentrationThe mixture was concentrated
2. custompurified on silica gel [2% MeOH in CH2Cl2 to 2% (2 N NH3-MeOH) in CH2Cl2)