Process For The Preparation Of Pyrimidine Compounds


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 -O.

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Document History
  • Publication: Apr 28, 2009
  • Application: Jun 7, 2005
    US US 53772305 A
  • Priority: Dec 9, 2003
    GB GB 0305359 W
  • Priority: Aug 7, 2003
    GB GB 0318515 A
  • Priority: Feb 17, 2003
    GB GB 0303589 A
  • Priority: Dec 16, 2002
    GB GB 0229243 A

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