Triethylamine → 5-Bromo-3-(4-(4-methylpiperazin-1-yl)phenylamino)picolinamide

Participants

Reaction Conditions

Reaction Steps

A solution of EXAMPLE 49A (1.8 g, 8.96 mmol) and 4-(4-methylpiperazin-1-yl)aniline (1.713 g, 8.96 mmol) in t-butanol (10 mL) was treated with triethylamine (1.87 mL, 13.43 mmol) was subjected to microwave irradiation (Biotage, Initiator) at 190° C. for 1.5 hours. The reaction mixture was concentrated and purified on silica gel with 0-10% methanol in dichloromethane. The collected material was taken into t-butanol (5 mL), treated with sodium t-butoxide (1.73 g, 18 mmol), and the reaction mixture was stirred at 90° C. for 2 hours. The mixture was concentrated and purified on silica gel with 3-13% methanol in dichloromethane to afford the title compound.

Provenance & Evidence