反应详情

Compound 218 (50 mg, 0.14 mmol), 4-fluoro-2-trifluoromethyl-benzoyl chloride (49 mg, 0.22 mmol), and DIEA (0.07 mL, 0.43 mmol) were dissolved in dioxane (2 mL) and stirred for 1 h at room temperature. The reaction was quenched with H2O, diluted with EtOAc, and filtered through an Extrelut column. The column was washed with EtOAc, and the filtrate was concentrated. The crude product was purified via Biotage eluting with a gradient of 0 to 100% EtOAc in hexanes to provide 219 (28 mg, 36% yield) as a tan solid. LC-MS (M+H=536, obsd.=536).

1. customThe reaction was quenched with H2O
2. additiondiluted with EtOAc
3. filtrationfiltered through an Extrelut column
4. washThe column was washed with EtOAc
5. concentrationthe filtrate was concentrated
6. customThe crude product was purified via Biotage
7. washeluting with a gradient of 0 to 100% EtOAc in hexanes