Trifluoroacetic acid → HCID 86708622, compound

Participants

Reaction Conditions

Reaction Steps

(+/−)-2-((3-((3R,4R)-4-amino-3-hydroxypiperidin-1-yl)-2-chloro-5-cyanophenyl)amino)-4-(ethyl(4-methoxybenzyl)amino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile (390 mg, 0.681 mmol) was mixed with anisole (0.372 mL, 3.40 mmol) and DCE (3 mL). TFA (1.049 mL, 13.61 mmol) was added and the mixture was stirred at 25° C. for 1 hr. The mixture was concentrated to dryness under high-vac. 30 ml 2N NH3/MeOH was added and stirred for 30 min. The white precipitate was collected by filtration and washed with 20 ml cold MeOH, ether, and dried under air-suction for 2 hrs to give rac-2-((3-((3R,4R)-4-amino-3-hydroxypiperidin-1-yl)-2-chloro-5-cyanophenyl)amino)-4-(ethylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile (193 mg).

Provenance & Evidence