Trifluoroacetic acid → 6-[[2-(4-Cyclopropylsulfonylphenyl)-2-(2,4-difluorophenoxy)acetyl]amino]pyridine-3-carboxylic acid

Participants

Reaction Steps

To a solution of tert-butyl 6-[[2-(4-cyclopropylsulfonylphenyl)-2-(2,4-difluorophenoxy)acetyl]amino]pyridine-3-carboxylate (Example A7; 1.6 g, 2.94 mmole) in DCM (5 mL) was added TFA (7 mL) dropwise at 0° C. Reaction mixture was stirred at rt for 3 hr. TFA was removed invaccuo, residue was neutralised using sat.NaHCO3 solution, extracted with ethyl acetate (3×25 mL) washed with brine, dried over anhydrous sodium sulfate and concentrated. Crude solid was triturated in diisopropyl ether and filtered washed with diisopropyl ether to afford pure product (1.2 g).

Provenance & Evidence