反应详情

4-Nitrophenyl chloroformate (59 mg, 0.29 mmol) was added to a solution of 3-((4-(4-amino-2-fluorobenzoyl)piperazin-1-yl)methyl)-N-tertbutylbenzamide (100 mg, 0.24 mmol) in acetonitrile (10 mL). After stirring at room temperature for 1 hour, cyclopropylmethylamine (126 μL, 1.21 mmol) was added. After 2 hours stirring, the reaction was purified by strong cation exchange chromatography, eluting macroporous polystyrene sulfonic acid with 2N ammonia in methanol. The resulting solution was concentrated under vacuum and purified by basic reverse phase HPLC to afford the title compound as a white solid (10 mg).

1. stirringAfter 2 hours stirring
2. customthe reaction was purified by strong cation exchange chromatography
3. washeluting macroporous polystyrene sulfonic acid with 2N ammonia in methanol
4. concentrationThe resulting solution was concentrated under vacuum
5. custompurified by basic reverse phase HPLC