反应详情

Benzyl chloroformate (3 mL, 21.5 mmol) was added to a mixture of 1-(5-amino-2-fluorophenyl)ethanone (3 g, 19.6 mmol) and tetrabutylammonium bromide at room temperature. The reaction was stirred at room temperature for 24 hours, the crude was treated with AcOEt (50 mL) and H2O (50 mL), the organic phase was separated and evaporated in vacuo. The crude was purified by column chromatography (silica gel; MeOH/DCM). The desired fractions were collected and the solvents evaporated in vacuo to afford intermediate A40 as a cream solid (4.7 g, 84%). LCMS: 286 [M−H]−; Rt: 2.81 min (method 3).

1. customthe organic phase was separated
2. customevaporated in vacuo
3. customThe crude was purified by column chromatography (silica gel; MeOH/DCM)
4. customThe desired fractions were collected
5. customthe solvents evaporated in vacuo