Acetamide → N-(4-{[3-(4-tert-butylphenyl)-5,5-dimethyl-2,4-dioxoimidazolidin-1-yl]methyl}pyridin-2-yl)acetamide

関与物質

反応条件

反応手順

To a solution of 400 mg of 3-(4-tert-butylphenyl)-1-[(2-chloropyridin-4-yl)methyl]-5,5-dimethylimidazolidine-2,4-dione obtained in stage a) below in 12 mL of dioxane are successively added, under argon, 23.3 mg of palladium diacetate, 72 mg of (9,9-dimethyl-9H-xanthene-3,6-diyl)bis(diphenylphosphine)[Xantphos], 1.18 g of caesium carbonate and 153 mg of acetamide. After heating for one hour at a temperature in the region of 90° C. and chromatography on a column of silica, eluting with a mixture of diethyl ether/ethyl acetate (gradient up to 100% of ethyl acetate), 370 mg of N-(4-{[3-(4-tert-butylphenyl)-5,5-dimethyl-2,4-dioxoimidazolidin-1-yl]methyl}pyridin-2-yl)acetamide are obtained in the form of white crystals, the characteristics of which are as follows:

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