Trifluoroacetic acid → (+/-)-4'-(5-chloro-4-(2-oxoazepan-3-ylamino)pyrimidin-2-ylamino)-5'-fluoro-N,2'-dimethylbiphenyl-4-carboxamide

Participants

Reaction Conditions

Reaction Steps

A mixture of 3-(2,5-dichloropyrimidin-4-ylamino)azepan-2-one (Intermediate 16, 28 mg, 0.10 mmol), 4′-Amino-5′-fluoro-N,2′-dimethylbiphenyl-4-carboxamide (Intermediate 17, 31 mg, 0.12 mmol, 1.2 equiv.) and TFA (37 μL, 57 mg, 0.50 mmol, 5 equiv.) in 2-propanol (3 mL) is stirred in a sealed tube at 100° C. for 48 h. The resulting solution is concentrated and then purified by preparative RP-HPLC to afford (±)-4′-(5-chloro-4-(2-oxoazepan-3-ylamino)pyrimidin-2-ylamino)-5′-fluoro-N,2′-dimethylbiphenyl-4-carboxamide; ESMS m/z 497.2 (M+H+).

Provenance & Evidence