反应详情

To the mixture of 1-(5-bromo-2-fluoro-phenyl)-2,2-difluoro-ethanone (6.0 kg, 23.7 mol) and (S)-(−)-tert-butanesulfinamide (3.3 kg, 27.2 mol) were added toluene (73 L) with stirring at ambient temperature. After 5 min, titanium ethoxide (6.5 kg, 28.5 mol) was added and the mixture was heated to 50˜55° C. The mixture was stirred at 50˜55° C. for 3 h and allowed to cool to ambient temperature before concentration in vacuo. The resulting crude product was used directly in next chemical transformation without further purification. ESIMS: 356 [(M+H)+].

1. temperaturethe mixture was heated to 50˜55° C
2. stirringThe mixture was stirred at 50˜55° C. for 3 h
3. temperatureto cool to ambient temperature before concentration in vacuo
4. customThe resulting crude product was used directly in next chemical transformation without further purification