反应详情

温度

50 °C

4-(4-Fluorophenyl)piperidine hydrochloride (63 mg, 0.29 mmol) was taken up in 3 mL of dry THF, neutralized with diisopropylethylamine (50 μL, 0.29 mmol) and cooled on an ice-water bath. [(4S)-4-metyl-2,5-dioxo-imidazolodin-4-yl]methanesulfonyl chloride (80 mg, 0.35 mmol) was added and after stirring for 10 min, diisopropylethylamine (50 μL, 0.29 mmol) was added and the reaction mixture was stirred at ambient temperature until LC-MS (APCD) indicated consumption of the amine. The reaction mixture was evaporated and the residue taken up in EtOH and heated to 50° C. and allowed to cool before water was added. The precipitated product was collected and washed with EtOH/water and dried in vacuum to yield 87 mg.

1. temperaturecooled on an ice-water bath
2. stirringthe reaction mixture was stirred at ambient temperature until LC-MS (APCD)
3. customconsumption of the amine
4. customThe reaction mixture was evaporated
5. temperatureto cool before water
6. additionwas added
7. customThe precipitated product was collected
8. washwashed with EtOH/water
9. customdried in vacuum
10. customto yield 87 mg