反应详情

1-(2-Fluorophenyl)ethanone (170 g, 1.23 mol), dimethylamine (137 g, 1.72 mol), and paraformaldehyde (55 g, 1.85 mol) were suspended in ethanol (500 mL), then concentrated HCl (3 mL) was added, and the mixture was heated to reflux overnight. The solvent was removed under vacuum. The residue was washed with EtOAc for 3 times to give 3-(dimethylamino)-1-(2-fluorophenyl)propan-1-one (207 g, 88%), which was used for the next step without purification. 1H NMR (CDCl3): δ=2.69 (s, 6H), 2.52 (m, 4H), 7.30 (m, 2H), 7.66 (m, 1H), 7.96 (m, 1H).

1. temperaturethe mixture was heated
2. temperatureto reflux overnight
3. customThe solvent was removed under vacuum
4. washThe residue was washed with EtOAc for 3 times