反应详情

A solution of 1-(4-fluorophenyl)azepan-2-one (1.1 g, 5.3 mmol) was dissolved in THF (5 mL) and was added into LDA (11 mmol) at −78° C. and stirred for 5 minutes. Benzyl chloroformate (1.6 ml, 11 mmol) was added at −78° C. and the reaction warmed to ambient temperature. The solution was poured into ice and diluted with EtOAc (100 mL). The organic layer washed with brine, dried with Na2SO4, filtered and concentrated. The residue was purified by column chromatography (50% EtOAc in hexane) to afford the product (1 g, 55% yield) as brown oil.

1. additionThe solution was poured into ice
2. washThe organic layer washed with brine
3. dry with materialdried with Na2SO4
4. filtrationfiltered
5. concentrationconcentrated
6. customThe residue was purified by column chromatography (50% EtOAc in hexane)