The selective transalkylation of N-methyl tertiary amines with 3,4-dibromobutenolides is described.The N-methyl group of the parent tertiary amines was replaced by alkenyl units of the butenolides;and a series of butenolide-containing tertiary enamines were obtained in moderate to good yields.Interestingly,the product 2b has shown a promising anticancer activity against HeLa cell lines(IC50=0.19 mmol/L). The selective transalkylation of N-methyl tertiary amines with 3,4-dibromobutenolides is described. N-methyl group of the parent tertiary amines was replaced by alkenyl units of the butenolides; and a series of butenolide-containing tertiary enamines were obtained in moderate To good yields.Interestingly, the product 2b has shown promising radiation activity against HeLa cell lines (IC50 = 0.19 mmol / L).