反应详情

温度

100 °C

A mixture of ((2S,3R)-2-(aminomethyl)-3-methylpiperidin-1-yl)(5-methyl-2-(1H-pyrazol-1-yl)phenyl)methanone (30 mg, 96 μmol), 2-chloro-5-fluoropyrimidine (18 μl, 144 μmol) and anhydrous DIPEA (50 g, 288 μmol) in CH3CN (2 mL) was heated at 100° C. for 3 days. The mixture was cooled to rt and the solvent was removed in vacuo. The crude was dissolved in EtOAc and washed with satd. aq. NaHCO3, brine, and dried (MgSO4). The solvent was removed and the crude was purified by reverse-phase preparative HPLC to afford the title compound. MS (ESI) 409 (M+H).

1. temperatureThe mixture was cooled to rt
2. customthe solvent was removed in vacuo
3. dissolutionThe crude was dissolved in EtOAc
4. washwashed with satd
5. dry with materialaq. NaHCO3, brine, and dried (MgSO4)
6. customThe solvent was removed
7. customthe crude was purified by reverse-phase preparative HPLC