Disclosed is a 4-aminopyrimidine derivative used as an adenosine A2A receptor antagonist, having general structural formula (I). R1 is selected from halogen, cyano group, or trifluoromethyl; R2 is selected from pyrazolyl, pyrrolidyl, or pyrazolyl or pyrrolidyl substituted by one or more halogens or C1-3 alkyl groups; R3 is selected from oxazolyl, oxadiazole group, triazole group, or oxazolyl substituted by one or more halogens or C1-3 alkyl groups. The 4-aminopyrimidine derivative provided by the present invention has an obvious antagonistic action on a human-derived adenosine A2A receptor, and can be applied to compositions or combination products for treating diseases or pathological symptoms having responses to the A2A antagonistic action, in particular for treating neurodegenerative disease, extrapyramidal syndrome, depression, hyperkinetic syndrome, sleep disorder, anxiety disorder, diabetes, tumor and other diseases.