反应详情

Borontribromide (20 mg, 0.0001 mol) was added to a stirred solution of cyclopropanesulfonic acid [1-benzyl-7-(4-bromo-2-fluoro-phenylamino)-6-methyl-5-oxo-1,2,3,5-tetrahydro-imidazo[1,2-a]pyridin-8-yl]-amide (1A: 30 mg, 0.0001 mol) in DCM (3 mL) at 0° C. The resulting mixture was stirred at room temperature for 2 hours. The reaction mixture was monitored by TLC (100% ethylacetate). The reaction mixture was quenched with methanol and concentrated. The concentrate was partitioned between ethyl acetate and water. The organic layer was concentrated to afford the crude product. Purification by column chromatography on silica gel (4% methanol in DCM) afforded 7 mg of the product (28% yield).

1. customThe reaction mixture was quenched with methanol
2. concentrationconcentrated
3. customThe concentrate was partitioned between ethyl acetate and water
4. concentrationThe organic layer was concentrated
5. customto afford the crude product
6. customPurification by column chromatography on silica gel (4% methanol in DCM)