反应详情

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).

1. temperatureThe mixture was heated
2. temperatureto reflux for 2 hours
3. concentrationAfter this time the reaction was concentrated under reduced pressure
4. custompurified by silica chromatography