反应详情

53 μl (0.5 mmol) thiophene methane amine, 172 mg (0.5 mmol) HATU and 165 μl (1.2 mmol) NEt3 were added consecutively to a solution of 123 mg (0.4 mmol) 2-ethoxy-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid in THF (3 ml) and thereafter stirred for 16 h at RT. The solution was subsequently diluted with EtOAc 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. 116 mg (0.3 mmol, 72%) 2-ethoxy-4-methyl-N-(thiophene-2-yl-methyl)-7-(trifluoromethyl)-quinoline-3-carboxylic acid amide (example 2) was obtained as a residue. MS: m/z 395.1 [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