Triethylamine → N-tert-Butyl-3-((4-(3-chloro-4-(3-(cyclopropylmethyl)ureido)-2-fluorobenzoyl)piperazin-1-yl)methyl)benzamide

Participants

Reaction Steps

To a stirred solution of bis(trichloromethyl) carbonate (0.128 mmol, 38.1 mg) in dichloromethane (6 mL) was added a mixture of triethylamine (0.867 mmol, 0.121 mL, 88 mg) and 3-((4-(4-amino-3-chloro-2-fluorobenzoyl)piperazin-1-yl)methyl)-N-tert-butylbenzamide (0.347 mmol, 155 mg) in dichloromethane (6 mL). The mixture was heated to reflux for 2 hours before being cooled to room temperature. Cyclopropylmethylamine (0.694 mmol, 0.060 mL, 49.3 mg) was added and the mixture stirred for 2 hours. After this time the reaction was concentrated under reduced pressure and purified by silica chromatography to yield the title compound (17 mg).

Provenance & Evidence