Diisopropylethylamine → N-[4-Fluoropyrimidin-2-yl]-N-methylglycine, methyl ester

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Reaction Steps

To a solution of 2,4-difluoropyrimidine (J.Heterocyclic Chem. 1985, 22, 149) (4.48 g) in isohexane (50 ml) at 0° C. was added sarcosine methyl ester hydrochloride (5.39 g) followed by N,N-diisopropylethylamine (13.45 ml). After 5 minutes, the ice bath was removed and the reaction mixture allowed to stir at room temperature for 3 hours. The solvents were evaporated under reduced pressure and the residue purified by chromatography eluting with ethyl acetate/isohexane mixtures. The first and minor component of the mixture to be eluted was the subtitle compound. Yield 0.68 g.

Provenance & Evidence