Hydrochloric Acid → 7-(2-Fluoro-4-methylsulfanyl-phenylamino)-pyrrolo[1,2-c]pyrimidine-6-carboxylic acid

Participants

Reaction Conditions

Reaction Steps

To a solution of 7-(2-fluoro-4-methylsulfanyl-phenylamino)-pyrrolo[1,2-c]pyrimidine-6-carboxylic acid methyl ester (635 mg, 1.9 mmol) in dioxane (8 mL) and water (2.5 mL) was added lithium hydroxide monohydrate (161 mg, 3.8 mmol). The reaction was stirred at 55° C. for 2 hours then cooled to room temperature. Aqueous hydrochloric acid (1M) was added dropwise until pH˜3. The reaction mixture was extracted twice with ethyl acetate (2×10 mL). The combined organic fractions were washed with brine, dried (MgSO4) and concentrated in vacuo to give the title compound as a dark brown solid (600 mg, 99%). LCMS (Method B): RT=3.20 min, M+H+=318.

Provenance & Evidence