The present disclosure provides a vinylation coupled derivative of β-elemene, and a preparation method and use thereof in preparation of an antitumor drug. The present disclosure provides a vinylation coupled derivative of β-elemene having a structure shown in Formula (I), a pharmaceutical composition and a hydrate including a compound shown in Formula (I), as well as an isotopic derivative, a chiral isomer, a variant, a salt, a prodrug, and a preparation of the compound shown in Formula (I). The present disclosure further provides a preparation method and use of the vinylation coupled derivative of β-elemene, and an inhibitory activity of the derivative on proliferation of various tumor cell lines. The vinylation coupled derivative of β-elemene is expected to be an antitumor drug candidate for treating colon cancer and lung cancer.