反应详情

4-Amino-3-fluorobenzoic acid (500 mg, 3.22 mmol), N-tert-butyl-3-(piperazin-1-ylmethyl)benzamide (888 mg, 3.22 mmol), N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (926 mg, 4.83 mmol, EDCl) and triethylamine (984 mg, 898 μl, 6.44 mmol) were combined and stirred in acetonitrile (10 mL) at room temperature overnight (under nitrogen). The reaction was concentrated under reduced pressure. The residue was taken up in dichloromethane (30 mL) and washed with water. The organic phase was dried over sodium sulfate and concentrated under vacuum. The residue was purified by silica chromatography (eluting with a solvent gradient from dichloromethane to 4% methanol/dichloromethane) to give the title compound (355 mg).

1. concentrationThe reaction was concentrated under reduced pressure
2. washwashed with water
3. dry with materialThe organic phase was dried over sodium sulfate
4. concentrationconcentrated under vacuum
5. customThe residue was purified by silica chromatography (
6. washeluting with a solvent gradient from dichloromethane to 4% methanol/dichloromethane)