反应详情

To a solution of (S)—N-(1-(3-(4-chloro-1-methyl-3-(methylsulfonamido)-1H-indazol-7-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2,2,2-trifluoroacetamide (57B, 8.0 g, 13.61 mmol) in DCM (70 mL) was added mCPBA (3.659 g, 16.33 mmol) in 4 portions over a 15 minute period. The reaction mixture was stirred at room temperature for 16 hours. Upon completion, the reaction was quenched with 1M aqueous NaHSO3 and saturated aqueous NaHCO3. The organic layer was collected and the aqueous layer was extracted an additional time with DCM. The combined organic layers were dried over Na2SO4, filtered, concentrated in vacuo, and purified by silica gel column chromatography, eluting with 50-100% EtOAc in hexanes to give the title compound. MS (m/z) 604.10 [M+H]+.

1. customUpon completion, the reaction was quenched with 1M aqueous NaHSO3 and saturated aqueous NaHCO3
2. customThe organic layer was collected
3. extractionthe aqueous layer was extracted an additional time with DCM
4. dry with materialThe combined organic layers were dried over Na2SO4
5. filtrationfiltered
6. concentrationconcentrated in vacuo
7. custompurified by silica gel column chromatography
8. washeluting with 50-100% EtOAc in hexanes