Benzene → HCID 86607940, compound

Participants

Reaction Conditions

Reaction Steps

To a mixture of 2-(4-cyanophenylamino)-2-(3-ethoxy-4-isopropoxyphenyl)acetic acid (US2004242585, which is incorporated herein by reference) (525 mg, 1.48 mg) and benzene amideoxime (242 mg, 1.78 mmol) in 10 mL CH2Cl2/DMF (9:1) at 0° C., were added HOAt (242 mg, 1.78 mmol), DIC (0.279 mL, 1.78 mmol) and TEA (0.248 mL, 1.78 mmol). The mixture was stirred at 0° C. for 15 min, then at rt for 6 h. The mixture was diluted with EtOAc, washed with H2O, 1 N HCl, H2O, sat. NaHCO3 and brine, dried (Na2SO4) and concentrated. The crude product was purified by flash chromatography (0 to 100% EtOAc/hexanes gradient) to afford 700 mg of Intermediate 187.1 as a white solid.

Provenance & Evidence