反应详情

温度

85 °C

Combine (S)-6-fluoro-3-(4-oxiranylmethoxy-phenyl)-benzo[d]isoxazole (150 mg, 0.526 mmol) dissolved in dimethylformamide (˜2 mL) and add 0.13 M solution of 4-benzylpiperidine in ethanol (˜4 mL) and heat for 10 hours at 85° C. Concentrate and purify the reaction mixture by flash (silica) chromatography on a Water's Sep-Pak 5 g silica cartridge using a graded solvent mixture of dichloromethane to 10% methanol in dichloromethane to give the title compound (169.9 mg, 70% Yield). Purity by LC/MS=99%, [M+H]+=461.

1. concentrationConcentrate
2. custompurify the reaction mixture by flash (silica) chromatography on a Water'
3. additiona graded solvent mixture of dichloromethane to 10% methanol in dichloromethane