The invention discloses a laminine ester bromo oxamide derivative with anticancer activity and a composition thereof. The preparation method includes the steps of conducting backflow on laminine hydrochloride in thionyl chloride, adding methyl alcohol to conduct backflow again, steaming excess solvent, and regulating to neutral until white precipitate is dissolved out; filtering, using glacial alcohol and diethyl ether to wash, and conducting vacuum drying to obtain a white solid product; dissolving N-(5-bromine-2-hydroxyl aniline) ethyl oxalyl in an absolute ethyl alcohol solution, slowly adding drop by drop into anhydrous THF which dissolves prepared 6-N,N,N-trimethyl-2-carbamyl methylamine hydrochloride, conducting temperature reaction, and regulating the solution to neutral with dilutehydrochloric acid or a dilute hydrobromic acid solution until white precipitate is dissolved out; filtering, taking the precipitate to conduct recrystallization with ethyl alcohol, and conducting vacuum drying to obtain a target product. According to the laminine ester bromo oxamide derivative with anticancer activity and the composition thereof, through the introduction of a brominated ring structure, the cytotoxic activity of laminine to tumor cell strains in vitro can be enhanced.