The invention relates to a synthetic method for gizzerosine and belongs to the technical field of medicines. According to the synthetic method provided by the invention, the steric hindrance of an end amino of lysine is different from that of an alpha-site amino, directly reacts with 4-(2-chloroethyl) imidazole to synthesize a target product through three-step reactions: histamine hydrochloride hydroxylation , chloro reaction and condensation. The method is simple and fast, is suitable for large-scale synthesis, and can be widely applied to related scientific research fields such as toxicology and metabolic experiments.