反应详情

温度

100 °C

Methyl 2-bromo-2-(4-methoxyphenyl)acetate (1.10 g, 4.25 mmol), DIPEA (0.89 mL, 5.09 mmol), and aniline (0.43 mL, 4.67 mmol) are dissolved in acetonitrile (12 mL). The reaction is heated for 18 minutes at 100° C. under microwave irradiation. Acetonitrile is evaporated and the residue is diluted with DCM and washed with water and brine, dried over Na2SO4, filtered and evaporated to dryness. The crude is purified by flash chromatography (Petroleum Ether/EtOAc=9/1) to give intermediate I139 as a yellow oil (745 mg, 65% yield).

1. customAcetonitrile is evaporated
2. additionthe residue is diluted with DCM
3. washwashed with water and brine
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. customevaporated to dryness
7. customThe crude is purified by flash chromatography (Petroleum Ether/EtOAc=9/1)