The invention discloses 2,4,6-trisubstituted pyrimidine compounds containing 1,2,3-triazole, a preparation method and application thereof in preparation of medicine and belongs to the field of medicinal chemistry. A pyrimidine parent nucleus and a 1,2,3-triazole activity unit are combined by using classical click chemistry to simply and efficiently synthesize the 2,4,6-trisubstituted pyrimidine compounds containing 1,2,3-triazole in an environment-friendly manner. The 2,4,6-trisubstituted pyrimidine compounds containing 1,2,3-triazole have a structure general formula as shown in the specification. In vitro anticancer activity tests show that the compounds have a certain inhibition effect on many tumor cells including EC-109, MCF-7, MGC-803 and B16 and can be applied to preparation of an antitumor medicine, as a further developed candidate or lead compound.