反应详情

To a solution of compound D of Example 1 (22 mg, 0.1 mmol), in a mixture of acetic acid and dichloromethane (1:1, 1 mL) were added 5-amino-N-cyclopropyl-2,4-difluorobenzamide (30 mg, 0.15 mmol) and NaBH(OAc)3 (30 mg, 0.2 mmol). The mixture was stirred at RT for 1 h. The reaction mixture was concentrated and the residue was purified by preparative RP HPLC. The appropriate fractions were collected and concentrated to remove methanol and saturated solution of NaHCO3 was added to precipitate out the desired product. The solid was filtered and dried in vacuo to give the title compound (6.5 mg) as a solid. LC/MS; (M+H)+=419.2

1. concentrationThe reaction mixture was concentrated
2. customthe residue was purified by preparative RP HPLC
3. customThe appropriate fractions were collected
4. concentrationconcentrated
5. customto remove methanol and saturated solution of NaHCO3
6. additionwas added
7. customto precipitate out the desired product
8. filtrationThe solid was filtered
9. customdried in vacuo