反应详情

To a suspension of 4-amino-3-(trifluoromethoxy)benzoic acid (900 mg, 4 mmol) in dichloromethane (60 ml) TBTU (1.9 g, 6 mmol) and DIPEA (1.04 ml, 6 mmol) were added. The mixture was stirred at room temperature for 30 minutes. Then 1-methylpiperidin-4-amine (513 mg, 4.5 mmol) was added and the reaction was stirred for an additional 3 h. The solution was washed with water and the organic phase was dried over anhydrous Na2SO4. The crude was purified by flash chromatography (DCM/MeOH/NH3aq, 9:1:0.5), to give the title compound (900 mg, 71%), as an orange solid.

1. additionwere added
2. stirringthe reaction was stirred for an additional 3 h
3. washThe solution was washed with water
4. dry with materialthe organic phase was dried over anhydrous Na2SO4
5. customThe crude was purified by flash chromatography (DCM/MeOH/NH3aq, 9:1:0.5)