反应详情

A mixture of 4-chloro-6-fluoro-2-(trifluoromethyl)quinoline (1 g, 4.01 mmol) and NH3 (3 mL) in ethylene glycol (20 mL) is prepared at −78° C. in a sealed tube. After warming up to room temperature, the sealed tube is gradually heated to 100° C. overnight. After cooling to −78° C., the sealed tube is opened and the contents are concentrated by rotary evaporator. The residue is purified by flash chromatography on silica gel (1:3 EtOAc/hexanes) to give 4-amino-6-fluoro-2-(trifluoromethyl)quinoline as a light yellow solid.

1. customis prepared at −78° C. in a sealed tube
2. temperaturethe sealed tube is gradually heated to 100° C. overnight
3. temperatureAfter cooling to −78° C.
4. concentrationthe contents are concentrated by rotary evaporator
5. customThe residue is purified by flash chromatography on silica gel (1:3 EtOAc/hexanes)