反应详情

To a solution of methyl 5-(ethyl{[4-(methyloxy)phenyl]methyl}amino)-2-fluoro-3-(2-oxo-1-pyrrolidinyl)benzoate (D155) (7 g, 17.5 mmol, 1 equiv) in EtOH (150 ml) was added 10% palladium on charcoal (50% wet, 1.4 g, 10% w/w) and the resulting mixture was stirred under an atmosphere of hydrogen (1 atm) for 3 h. The catalyst was filtered off through a pad of celite and the solution concentrated in vacuo. The residue was triturated with AcOEt/iso-hexane to give methyl 5-(ethylamino)-2-fluoro-3-(2-oxo-1-pyrrolidinyl)benzoate (B118) (4.8 g, 98%) as a pale greenish solid which was used in the next step without further purification. [M+H]+=281.2, RT=2.35 min.

1. filtrationThe catalyst was filtered off through a pad of celite
2. concentrationthe solution concentrated in vacuo
3. customThe residue was triturated with AcOEt/iso-hexane