Cesium fluoride → 2-(((2S,3R)-1-(3-Fluoro-2-(pyrimidin-2-yl)benzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione

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Reaction Conditions

Reaction Steps

A mixture of 2-(((2S,3R)-1-(3-fluoro-2-iodobenzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione (0.493 g, 0.974 mmol), 2-(tributylstannyl)pyrimidine (0.4 g, 1.07 mmol), CsF (0.3 g, 1.948 mmol), CuI (0.0185 g, 0.098 mmol) and Pd(PPh3)4 (0.112 g, 0.098 mmol) in DMF (5 mL) was degassed and heated at 100° C. oil bath for 16 h. The solvent was removed in vacuo to obtain the crude which was purified by silica gel chromatography (0˜100% EtOAc/hexanes) to yield the title compound as a white solid (0.331 g, 75%). MS (ESI) 459 (M+H).

Provenance & Evidence