反应详情

温度

50 °C

311 μl (2.7 mmol) 4-fluorobenzylamine, 941 mg (2.5 mmol) HATU and 1 ml (7.2 mmol) NEt3 were added consecutively to a solution of 740 mg (2.5 mmol) 4-methyl-2-propyl-7-(trifluoromethyl)quinoline-3-carboxylic acid in THF (19 ml) and the mixture was then stirred for 72 h at 50° C. The mixture was then diluted with EA and washed with a 4N aq. NH4CL sol., a 1M aq. Na2CO3 sol. and brine. The organic phase was dried over MgSO4, filtered through silica gel and concentrated in a vacuum. After CC (EtOAc/hexane 1:1) of the residue, 770 mg (1.9 mmol, 76%) N-[(4-fluorophenyl)-methyl]-4-methyl-2-propyl-7-(trifluoromethyl)-quinoline-3-carboxylic acid amide (example 3) was obtained. MS: m/z 405.2 [M+H]+.

1. washwashed with a 4N aq. NH4CL sol.
2. dry with materialThe organic phase was dried over MgSO4
3. filtrationfiltered through silica gel
4. concentrationconcentrated in a vacuum