反应详情

温度

100 °C

Ethyl 2-(methylsulfonyloxy)-2-(thiophen-2-yl)acetate (I27) (5.7 g, 21.6 mmol), aniline (2.16 ml, 23.7 mmol) and DIPEA (4.52 ml, 25.9 mmol) were dissolved in acetonitrile (20 ml) to give a yellow solution which was heated under microwave irradiation into a sealed vial at 100° C. for 15 minutes. Conversion complete by UPLC/MS-UV. The solvent was evaporated, and the residue was dissolved in DCM and washed with water and brine, dried (Na2SO4), filtered and evaporated to dryness. The resulting crude was purified by flash chromatography (Petroleum ether/EtOAc=85/15) to get desired compound as a solid (4.33 g, 77% yield).

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