Patent ID: 8841447

Claim:
A process for producing a pyrimidin-dione derivative represented by the structure of formula (I): wherein: R 1 and R 5 are each independently H or (C 1 -C 10 )alkyl, R 2 is CH 2 Ar, and R 3 and R 4 together with the nitrogen to which they are attached form a 4, 5, 6 or 7 membered ring, which may be unsubstituted or substituted; the process comprising the steps of: 1) reacting a urea derivative of Formula (VIII): with malonic acid or its derivatives of formulae RO 2 CCH(R 5 )CO 2 Ror RO 2 CCH(R 5 )CN, so as to form a compound of formula (VII) or (VII-A): wherein R is H, (C 1 -C 10 )alkyl, phenyl or N-oxysuccinimidyl ester, wherein each of the alkyl or phenyl may be unsubstituted or substituted; 2) reacting compounds (VII) or (VII-A) with a reagent that introduces or forms the group X, so as to form a compound of the formula (II): wherein X is a leaving group; and 3) reacting compound (II) with a reagent of Formula (III): HNR 3 R 4 so as to form the compound of Formula (I)