Process for the Preparation of Pyrimidine Compounds

摘要

A process for the preparation of a compound of Formula (I) and intermediates useful therein are provided. The process comprises reacting a compound of formula R¹-CO-CH₂-E with a compound of formula R²-CHX¹X² in the presence of a compound of formula R³R⁴N-C(-NH)NH₂ and a catalyst, thereby to form a dihydropyrimidine; and oxidising the dihydropyrimidine to form the compound of Formula ( 1 ). R¹ is H or an alkyl group; R² is H, an alkyl or aryl group; R³ and R⁴ are each independently H, alkyl or aryl, or R³ and R⁴ are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, and aryl group or an electron withdrawing group; and X¹ and X² are each independently leaving groups, or X¹ and X² together represent -