Disclosed herein is a process for preparaing amine and acetylene substituted [1,2,4] triazole [1,5,-a] pyrimidine compounds of general formula (I), wherein the substituents are as defined within the specification, the process comprising: coupling an aromatic halide of formula (1) with an alkyne of formula (2) in the presence of a base, a palladium catalyst and a copper (I) salt, to provide a compound of (3), or deprotonating a compound of formula (3a) in the presence of base and treating the resulting anion with ketones or aldehydes of formula (4) in a solvent, to provide a compound of formula (3b).
