反应详情

To 3-(methylsulfonyl)-5-(trifluoromethyl)benzoic acid (1 g, 3.73 mmol, example 1, intermediate d) was added N,N-dimethylformamide (27.3 mg, 28.9 μL, 373 μmol) and thionyl chloride (8.87 g, 5.44 ml, 74.5 mmol) and the suspension was heated to reflux for 30 min. A light brown solution was formed. To remove thionyl chloride, the light brown solid was diluted with toluene, followed by complete evaporation. This procedure was repeated two times to provide the desired compound as a colorless solid (1.1 g; 99%) which was pure enough for the next step without further purification.

1. temperaturethe suspension was heated
2. temperatureto reflux for 30 min
3. customA light brown solution was formed
4. customTo remove thionyl chloride
5. additionthe light brown solid was diluted with toluene
6. customfollowed by complete evaporation