Trifluoroacetic acid → HCID 68563994, compound

Participants

Reaction Steps

Trifluoroacetic acid (727 μL) was added at 0° C. to a dichloromethane (2.90 mL) solution of the tert-butyl 4-({6-[5-(methylsulfonyl)indolin-1-yl]pyrimidin-4-yl}oxy)piperidine-1-carboxylate (145 mg, 0.306 mmol) produced in Example 1, and the mixture was stirred at room temperature for 1 hour. The solvent was distilled off under reduced pressure. To a dichloromethane (3.70 mL) solution of the obtained residue and diisopropylethylamine (1.07 mL, 6.14 mmol), a dichloromethane (1.85 mL) solution of 1-butanesulfonyl chloride (72.0 mg, 0.461 mmol) was added at 0° C., and the mixture was stirred at 0° C. for 1 hour and then at 80° C. for 3 hours. The solvent was distilled off under reduced pressure. To the residue, methanol was added, and the deposit was collected by filtration. The obtained crude product was washed with methanol to obtain the title compound as white powder (125 mg, yield: 82%).

Provenance & Evidence