Patent ID: 6992187
Filing Date: 2006-01-31
Classification: A61P,C07D

Abstract:
1. A process for the preparation of a compound of the formula (IV) wherein R where alkyl, cycloalkyl and aryl are unsubstituted or substituted by at least one member selected from the group consisting of fluorine, chlorine, bromine, —CF R R where aryl, cycloalkyl and alkyl are optionally substituted once, twice or three times by a member selected from the group consisting of fluorine, chlorine, bromine, -cyano, —CF R R R in all its stereoisomeric forms admixtures thereof and its salts, comprising reacting the 5-nitropyrimidine of formula (V) with a primary amine of the formula (VI) to obtain a compound of the formula (VII), wherein R 1 , R 2 , R 3 , R 4 and R 5 are defined as above, reducing the compound of formula (VII) to a compound of the formula and cyclizing the compound of formula (VIII) to obtain a compound of formula (IV) by means of a tri(C 1 –C 4 ) alkyl orthoformate.