Citric Acid → AM-206 free acid

Participants

Reaction Steps

(5-{2-[(N-Benzyloxycarbonyl-N-ethyl-amino)-methyl]-4-trifluoromethyl-phenyl}-pyridin-3-yl)-acetic acid methyl ester (0.1 g, 0.2 mmol) in THF (2 mL), MeOH (0.5 mL), and H2O (0.5 mL) was treated with lithium hydroxide (0.03 g) and stirred at room temperature until no starting material was seen by analytical LCMS. The reaction was neutralized with citric acid to pH 4 and extracted with EtOAc, and the combined organic layers were washed with H2O, dried over MgSO4, filtered, and concentrated to give Compound 12.

Provenance & Evidence