p-Toluenesulfonic acid monohydrate → HCID 56644098, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-chloro-5-fluoro-N-(2,2,6,6-tetramethylpiperidin-4-yl)pyrimidin-4-amine hydrochloride (160 mg, 0.495 mmol, 1 equiv), 4-isopropyl-3-(1H-tetrazol-1-yl)benzenamine (121 mg, 0.594 mmol, 1.2 equiv), and para-toluenesulfonic acid monohydrate (75 mg, 0.396 mmol, 0.8 equiv) in IPA (3 mL) were heated to 100° C. for 3 hours. After cooling to ambient temperature, the crude mixture was quenched with 2M NH3/MeOH followed by concentrating to dryness. The crude product was purified by flash chromatography and eluted with DCM:2M NH3/MeOH (95:5) to provide the desired product (120 mg, 54%) as a white solid.

Provenance & Evidence