Methylamine → Ethyl 2-fluoro-4-(methylamino)-5-nitrobenzoate

Participants

Reaction Steps

A 2N solution of methylamine in THF (11.5 ml, 23.0 mmol) was added at −5° C. to ethyl-2,4-difluoro-5-nitro-benzoate (2.50 g, 10.8 mmol) in 20 ml THF and the cooling bath was removed. After 15 min at room temperature, the mixture was concentrated i.vac., 50 ml DCM were added, the organic phase was washed with water and dried with MgSO4. After concentration i.vac. the crude product was triturated with ethanol to give the cristalline product.

Provenance & Evidence