Process for preparing 5-fluoro-4-imino-3-methyl-1-(toluene-4-sulfonyl)-3,4-dihydro-1H-pyrimidin-2-one

Abstract

The present invention provides a process for preparing the compound 5-fluoro-4-imine-3-methyl-1-(phenyl-4-sulfonyl)-3,4-dihydro-1H-pyrimidin-2-one having the formula (I): comprising (a) reacting 5-fluorocytosine with compound having the formula (III): in the presence of at least one polar solvent and at least one base to obtain the compound having the formula (II) and (b) reacting compound having the formula (II) with dimethylsulphate (DMS), wherein R is hydrogen, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, alkylthio, haloalkylthio, amino, alkylamino, dialkylamino, alkoxycarbonyl, alkyl carbonyl, hydroxyalkyl, ester, acid halogen, —SH, —OH, —NH2, —NO2, —CN or CF3, and X is a halogen or —OSO2PhR.

Dependencies are inferred from the claim text.