Trifluoroacetic acid → 2-((2-Chloro-5-cyano-3-(4-hydroxybutan-2-yl)phenyl)amino)-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile

Participants

Reaction Conditions

Reaction Steps

2-((2-chloro-5-cyano-3-(4-hydroxybutan-2-yl)phenyl)amino)-4-(cyclopropyl(4-methoxybenzyl)amino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile (25 mg, 0.046 mmol) was taken up in DCE (0.5 mL) and anisole (10.06 μl, 0.092 mmol) was added, followed by TFA (0.142 mL, 1.842 mmol). The reaction was heated at 50° C. for 2 h. The solvent was removed in vacuo and the material dissolved in 2N NH3 in MeOH. The solution was stirred for 10 min to cleave the ester, and the solvent was removed in vacuo. The material purified by preparative HPLC. 2-((2-chloro-5-cyano-3-(4-hydroxybutan-2-yl)phenyl)amino)-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile (10.7 mg) was obtained.

Provenance & Evidence