Sodium Hydroxide → HCID 66620465, compound

Participants

Reaction Conditions

Reaction Steps

The mixture of polyphosphoric acid (4 g) and 2-(3-fluoro-4-(2-hydroxy-3-(methoxycarbonyl)phenylcarbamyl)phenyl)pyrrolidine-1-carboxylate (1.1 g, 2.23 mmol) was stirred at 180° C. for 0.5 h under nitrogen, and then cooled to 0° C. Water (50 mL) was added to the mixture and adjusted to pH=7 with sodium hydroxide at 0° C., the solution was extracted with ethyl acetate; the liquid layer was adjusted to pH=5, the water was evaporated under vacuum, the methanol was added, filtered, the solvent was dried over anhydrous sodium sulfate, evaporated to obtain 2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)benzo[d]oxazole-7-carboxylic acid (500 mg, yield 69%). LC-MS (ESI) m/z: 327 (M+1)+.

Provenance & Evidence