Patent ID: 8614320

Claim:
A process for preparing a 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound having the formula (3): in which R is selected from the group consisting of an alkyl group having from 1 to 10 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms, an aryl-alkyl group having an alkyl moiety of from 1 to 3 carbon atoms, an aryl group and a methylphenyl group, which comprises the steps of: (I) reacting an isobutyrylacetate ester of the following formula (5): wherein R is the same as above, with 4-fluorobenzaldehyde and urea in the presence of a protonic compound selected from the group consisting of an inorganic acid or a salt thereof, an organic sulfonic acid, an organic carboxylic acid and an alcohol; and a metal salt selected from the group consisting of copper(I) chloride, copper(II) chloride, copper(II) acetate, iron(II) chloride, iron(III) chloride, aluminum chloride, nickel(II) bromide, tin(VI) chloride, titanium tetrachloride, and magnesium bromide; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide having the formula (2): R′SO 2 X (2) in which R′ is selected from the group consisting of an alkyl group having from 1 to 10 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms, an aryl-alkyl group having an alkyl moiety of from 1 to 3 carbon atoms, an aryl group and a methylphenyl group, and X is a halogen atom, or an organic sulfonic anhydride having the formula (2a): (R′SO 2 ) 2 O (2a) in which R′ has the same meaning as above; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.