反应详情

温度

0 °C

A suspension of 4-bromo-2-fluoro-1-(trifluoromethoxy)benzene (582 g, 2247 mmol), Mg (54.6 g, 2247 mmol) and iodine in THF (10 mL) was heated at reflux for 2 h. The reaction was cooled to 0° C. and added to a solution of (E)-2-methyl-N-(oxazol-5-ylmethylene)propane-2-sulfinamide (300 g, 1498 mmol, step 1 of example 1) in toluene (10 mL) cooled to 0° C. The reaction was stirred at 0° C. for 30 min. The reaction was quenched with water and extracted with DCM. The organic layer was concentrated to afford crude N-((3-fluoro-4-(trifluoromethoxy)phenyl)(oxazol-5-yl)methyl)-2-methylpropane-2-sulfinamide (55) which was used without further purification.

1. temperaturewas heated
2. temperatureat reflux for 2 h
3. temperaturecooled to 0° C
4. customThe reaction was quenched with water
5. extractionextracted with DCM
6. concentrationThe organic layer was concentrated