The invention provides a cyclobutane-diamide compound with antitumor activity and a preparation method and application thereof. The structure formula of the compound is shown in the description, wherein R1 and R2 are hydrogen, alkane groups or halogen groups. The compound has very good inhibitory activity for VEGFR-2 kinase and can cut off an inductive signal channel of the VEGFR-2 kinase and restrain hyperplasia and migration of tumor cells by restraining the activity of the VEGFR-2 kinase, and therefore the compound can be applied to preparation of antitumor drugs. The preparation method of the compound has the advantages that raw materials are easy to get, reaction conditions are mild, operation is easy in the reaction process, and adopted reagents are low in price.