Hydrogen chloride-ethyl acetate → 5-(Methylsulfonyl)-1-(6-(piperidin-4-yloxy)pyrimidin-4-yl)indoline

Participants

Reaction Steps

A 4 N hydrochloric acid-ethyl acetate solution (9.45 mL) was added at 0° C. to an ethyl acetate (3.15 mL) suspension of tert-butyl 4-({6-[5-(methylsulfonyl)indolin-1-yl]pyrimidin-4-yl}oxy)piperidine-1-carboxylate (630 mg, 1.33 mmol) produced in Example 1 below, and the mixture was stirred for 1 hour. The solvent was distilled off under reduced pressure. To the obtained residue, a 1 N aqueous sodium hydroxide solution (20 mL) was added, and the deposit was collected by filtration and washed with water to obtain the title compound as white powder (489 mg, yield: 99%).

Provenance & Evidence