Acetonitrile → methyl 2-fluoro-5-nitro-4-[2-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-1-yl]benzoate

関与物質

反応手順

To a mixture of 4.10 g of methyl 2,4-difluoro-5-nitrobenzoate and 40 mL of acetonitrile was added 4.76 mL of triethylamine, and 2.60 g of 2-(tetrahydro-2H-pyran-4-yl)-1H-imidazole was gradually added thereto under ice-cooling, followed by stirring at room temperature for 4 hours. To the reaction mixture were added water and ethyl acetate, followed by extraction with ethyl acetate, the organic layer was washed with saturated brine and then dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The obtained residue was purified by silica gel column chromatography (chloroform/methanol) to obtain 3.84 g of methyl 2-fluoro-5-nitro-4-[2-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-1-yl]benzoate as a yellow solid.

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