反应详情

To a solution of 3-methoxy-5-methyl-4-oxo-4,5-dihydropyrazolo[1,5-a]quinoxaline-2-carboxylic acid (75 mg, 0.27 mmol) in DMF were added HOBT (46 mg, 0.3 mmol), EDC (76 mg, 0.4 mmol), DIEA (0.05 mL, 0.29 mmol), and 4-fluorobenzylamine (50 mg, 0.4 mmol). The reaction mixture was stirred at room temperature for 24 hours. The solvent was removed under reduced pressure and the residue was partitioned between EtOAc and aqueous sodium bicarbonate. The EtOAc layer was dried (MgSO4), filtered and the solvent was removed under reduced pressure. The residue was triturated in MeOH to give the product as a white solid. 1H NMR (400 MHz, d6-DMSO) δ 8.91 (t, J=5.9 Hz, 1H), 8.26 (d, J=8.0 Hz, 1H), 7.62 (d, J=7.8 Hz, 1H), 7.54 (t, J=7.9 Hz, 1H), 7.39-7.44 (m, 3H), 7.17 (t, J=8.9 Hz, 2H), 4.49 (d, J=6.1 Hz, 2H), 4.02 (s, 3H), 3.61 (s, 3H); ES MS (M+1)=381.

1. customThe solvent was removed under reduced pressure
2. customthe residue was partitioned between EtOAc and aqueous sodium bicarbonate
3. dry with materialThe EtOAc layer was dried (MgSO4)
4. filtrationfiltered
5. customthe solvent was removed under reduced pressure
6. customThe residue was triturated in MeOH