Pyridine → HCID 57625978, compound

Participants

Reaction Steps

To a solution of 100 mg of 1-[(2-aminopyrimidin-4-yl)methyl]-3-(4-tert-butylphenyl)-5,5-dimethylimidazolidine-2,4-dione obtained in stage f) of Example 1, in 3 mL of tetrahydrofuran, are added, at 0° C., 0.034 mL of pyridine and 0.045 mL of phenyl chlorocarbonate. The reaction mixture is stirred for 4.5 hours at room temperature and then diluted with ethyl acetate and washed with twice 30 mL of aqueous 1N hydrochloric acid solution, then with twice 30 mL of water, with twice 30 mL of saturated aqueous sodium hydrogen carbonate solution and finally with saturated aqueous sodium chloride solution. The organic phase is dried over magnesium sulphate, filtered and concentrated under reduced pressure. The residue is purified by chromatography on a column of silica, eluting with an ethyl acetate/cyclohexane mixture (62/38 by volume) to give 70 mg of phenyl (4-{[3-(4-tert-butylphenyl)-5,5-dimethyl-2,4-dioxo-imidazolidin-1-yl]methyl}pyrimidin-2-yl)carbamate in the form of a white powder, the characteristics of which are as follows:

Provenance & Evidence