Patent ID: 6559307
Filing Date: 2003-05-06
Classification: C07D

Abstract:
A process for the preparation of substituted pyrimidines of formula IA whereinR3 and R4 each independently represent a hydrogen atom, alkyl optionally substituted by phenyl, halogen, nitro, cyano, hydroxyl, C1-4-alkoxy, C1-4-haloalkoxy or C1-4-alkoxycarbonyl, or represents phenyl optionally substituted by halogen, nitro, cyano, hydroxyl, C1-4-alkyl, C1-4alkoxy, C1-4-haloalkyl, C1-4-haloalkoxy C1-4-haloalkylthio or halosulfanyl, and R1 represents C3-8 cycloalkyl optionally substituted by phenyl, halogen, nitro, cyano, amino, hydroxyl, C1-4-alkoxy, C1-4-haloalkoxy or C1-4-alkoxycarbonyl, or represents pyrazin-2-yl optionally substituted by halogen, nitro, cyano, amino, hydroxyl, C1-4-alkyl, C1-4-alkoxy, C1-4-haloalkyl, C1-4-haloalkoxy C1-4-haloalkylthio or halosulfanyl, R5 represent a halogen atom or a haloalkyl or haloalkoxy group and W-V represents Nâ€”CH, Sâ€”CH, Nâ€”CHâ€”CH, CHâ€”CHâ€”CH or Nâ€”N(R6), in which R6 represents a C1-4 alkyl group which comprises reacting an amidine of formula II, or a salt thereof with 3,3-dichloroacrolein in an inert solvent, in the presence of a base and in the presence of a compound of formula IVHâ€”Xâ€”R2â€ƒâ€ƒ(IV), wherein X denotes oxygen and R2 represents a group and which further comprises perparing the 3,3-dichloroacrolein by an in-situ hydrolysis of a 1,1,1,3-tetrachloro-3-alkoxypropane.