Methylboronic Acid → 3-{4-[4-(5-Fluoro-2,4-dimethylphenyl)piperazine-1-carbonyl]-3-methanesulfonylphenyl}oxazolidin-2-one

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Reaction Steps

To a mixture of 3-{4-[4-(2-chloro-5-fluoro-4-methylphenyl)piperazine-1-carbonyl]-3-methanesulfonylphenyl}oxazolidin-2-one (0.5 g) described in Preparation Example 14, methylboronic acid (479 mg), palladium (II) acetate (90 mg), 2-dicyclohexylphosphino-2′,6′-dimethoxybiphenyl (328 mg) and potassium fluoride (930 mg) was added tetrahydrofuran (12 mL), and the mixture was refluxed for 18 hr. After cooling, water was added to the reaction mixture, and the mixture was extracted with chloroform. The organic layer was washed with saturated brine, and the solvent was evaporated. The residue was purified by column chromatography (chloroform:methanol) to give the title compound (55 mg).

Provenance & Evidence