Ethanol → Ethyl 2-(5-amino-2-fluorophenyl)acetate

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-(5-amino-2-fluorophenyl)acetic acid (6.13 g, 36.2 mmol) in ethanol (15 mL) was added conc. sulfuric acid (2 mL) dropwise. The reaction mixture was stirred under N2 at 80° C. for 1 hr. After the reaction mixture was cooled to RT and neutralized with aqueous Na2CO3 to pH 7-8, the aqueous solution was extracted with ethyl acetate (3×100 mL). The combined organic layer was washed with brine, dried over Na2SO4 and evaporated under vacuum to afford ethyl 2-(5-amino-2-fluorophenyl)acetate as a yellow oil which was used for the next step without further purification (6.13 g, 95%).

Provenance & Evidence