1-Fluoro-2-nitrobenzene → (S)-2-(2-Nitro-phenylamino)-propionic acid tert-butyl ester

Participants

Reaction Steps

To a solution of 2-fluoronitrobenzene (1.0 g, 7.09 mmol) in DMF (5 mL) were added H-ALA-OTBU HCl (2.6 g, 14.2 mmol) and DIPEA (2.5 mL, 14.2 mmol). The reaction mixture was stirred at room temperature over the weekend. The reaction mixture was then diluted with ethyl acetate and washed with water (×4). The organic phase was then dried over Na2SO4 and concentrated to afford 1.8 g (95%) of the desired product as orange oil. The resulting residue was used for the next reaction without further purification.

Provenance & Evidence