Hydrochloric Acid → 2-({5-[(Azetidin-3-yloxy)methyl]-6-methylpyridin-2-yl}amino)-5-[2,6-difluoro-4-(1-hydroxy-1-methylethyl)phenyl]thiophene-3-carboxamide

Participants

Reaction Conditions

Reaction Steps

tert-Butyl 3-{[6-({3-(aminocarbonyl)-5-[2,6-difluoro-4-(1-hydroxy-1-methylethyl)phenyl]-2-thienyl}amino)-2-methylpyridin-3-yl]methoxy}azetidine-1-carboxylate (146 mg, 0.248 mmol) was suspended in acetonitrile (4 mL). Aqueous hydrochloric acid (3.7 mL of 1N, 3.7 mmol) was added, and the reaction was allowed to react at room temperature overnight. It was then heated to 50° C. for 5 hours. The mixture was cooled to room temperature, neutralized with 1 N aqueous sodium hydroxide and extracted with ethyl acetate (3×). The combined organic layers were dried over magnesium sulfate, filtered, and concentrated under reduced pressure to afford the title compound.

Provenance & Evidence