A mixture of 238 mg (0.6 mmol) 2-chloro-N-(3-fluorobenzyl)-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid amide, 146 mg (1.8 mmol) ethylamine hydrochloride, 469 μl (2.7 mmol) DIPEA and MeCN (1,6 ml) was heated in a sealed vessel with microwave radiation to 180° C. for 2 h. After cooling to RT, dilution was carried out with EtOAc (30 ml) and a 2M aq. NaOH sol. (5 ml). The organic phase was then separated, washed with water and brine, dried over MgSO4 and concentrated in a vacuum. After column chromatographic separation (silica gel, EtOAc/hexane 3:7) of the residue, 188 mg (0.5 mmol, 77%) 2-ethylamino-N-[(3-fluorophenyl)-methyl]-4-methyl-7-(trifluoromethyl)-quinoline-3-carboxylic acid amide (example 1) was obtained. MS: m/z 406.1 [M+H]+.
