SYNTHESIS OF 4-AMINO-PYRIMIDINES

摘要

Process for the manufacture of a compound of the structure (I) with R¹ = hydrogen, alkyl (C1 - C10, linear, cyclic or branched, aliphatic or aromatic), NR'R" (wherein R' and R" are independently selected from H, alkyl [C1 - C10, linear, cyclic or branched, aliphatic or aromatic] and R² = CH₂R³ wherein R³ is selected from NHR1"' (with R"' = C(O)H, C(O)CH₃, C(O)alkyl, CH₂C₆H₂(OMe)₃ or other saponifiable residues), alkyl (C1 - C10, linear, cyclic or branched) aromatic residues, heteroaryl residues, substituted aryl residues, e. g. 3,4,5-trimethoxy-phenyl) wherein 1 equivalent of an a-formyl-propionitrile salt is reacted with 0.75 to 2 equivalents of an acetamidine salt in the presence of a Lewis acid.