反应详情

温度

100 °C

Ethyl 2-(methylsulfonyloxy)-2-(thiophen-2-yl)acetate (I87) (5.7 g, 21.6 mmol), aniline (2.16 mL, 23.7 mmol) and DIPEA (4.52 mL, 25.9 mmol) are dissolved in acetonitrile (20 mL) to give a yellow solution which is heated under microwave irradiation into a sealed vial at 100° C. for 15 minutes. Conversion complete by UPLC/MS-UV. Solvent is evaporated and the residue is dissolved in DCM and washed with water and brine, dried (Na2SO4), filtered and evaporated to dryness. The resulting crude is purified by flash chromatography (Petroleum ether/EtOAc=85/15) to get desired compound as a yellow solid (4.33 g, 77% yield).

1. customto give a yellow solution which
2. customSolvent is evaporated
3. dissolutionthe residue is dissolved in DCM
4. washwashed with water and brine
5. dry with materialdried (Na2SO4)
6. filtrationfiltered
7. customevaporated to dryness
8. customThe resulting crude is purified by flash chromatography (Petroleum ether/EtOAc=85/15)