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Ketone to Difluoro

(DAST)







Examples:


Example 1



To a solution of the SM (800 mg, 2.8 mmol) in DCM (10 mL) was added DAST (1.36 g, 8.4 mmol) at RT, and the reaction mixture was stirred at RT overnight. The mixture was poured into sat aq NaHCO3 (80 mL) with stirring at RT, then was extracted with DCM (2 x 40 mL). The combined organics were dried, concentrated, and purified by silica gel column chromatography (20:1 PE/EtOAc) to provide the product as a colorless oil. [820 mg, 95%]


[Patent Reference: WO2016011930, page 152, (15.7 MB)]