反应详情

1.0M Solution of borontribromide in DCM (6.4 mL, 6.4 mmol) was added to a solution of 5-amino-6,7-difluoro-1-(2-fluoro-4-iodo-phenyl)-4-methoxy-1,3-dihydro-benzoimidazol-2-one (I-11a: 1.4 g, 3.2 mmol) in DCM (50 mL) at 0° C. and the resulting mixture was stirred at room temperature overnight. The reaction was monitored by TLC (80% ethyl acetate in hexane). The reaction mixture was quenched with water and stirred for 1 hour. The aqueous layer was extracted with ethyl acetate (100 mL×2). The combined organic layers were washed with brine, dried over anhydrous Na2SO4 and concentrated to afford 1.15 g of the product (85.1% yield).

1. customThe reaction mixture was quenched with water
2. stirringstirred for 1 hour
3. extractionThe aqueous layer was extracted with ethyl acetate (100 mL×2)
4. washThe combined organic layers were washed with brine
5. dry with materialdried over anhydrous Na2SO4
6. concentrationconcentrated