The invention relates to an open-loop maleimide derivative utilizing click chemosynthesis and having kinase inhibitory activity. The structural general formula of the open-loop maleimide derivative is shown in A. In the formula, R1 and R2 can be a hydrogen atom, alkyl, a naphthenic base, heterocyclic alkyl, heterocyclic alkyl, alkenyl, cyclohexenyl, heterocyclic alkenyl, heterocyclic alkenyl, chain alkynyl, heterocyclic alkynyl, heterocyclic alkenyl, aryl, heterocyclic aryl or glycosyl, wherein R3 is the hydrogen atom or methyl. The open-loop maleimide derivative comprises a compound obtained through performing substitution derivatization or bridging derivatization on the R1 and/or the R2 alternately and repeatedly, and also comprises a compound obtained through performing single-bond linked derivatization on the R1 and the R2. The compounds can be applied to preparing drugs for treating neurodegenerative diseases and cancers.