The invention discloses a synthesis method and application of a
bismuth-based chelate X-
ray contrast agent. The method comprises the following steps: in N, N-
dimethylacetamide, reacting cycleanine with halogenated
carboxylic ester under an alkaline condition to obtain a first intermediate; reacting the first intermediate with 4, 4-dimethyl-3, 5, 8-trioxabicyclo [5.1. 0]
octane under an alkaline condition, and acidifying to obtain a second intermediate; the second intermediate and a
bismuth agent are subjected to a
chelation reaction under the hydrothermal condition and purified, and the
bismuth-based chelate contrast agent 10-(1, 3, 4-trihydroxybutyl-2-yl)-1, 4, 7, 10-tetraazacyclododecane-1, 4, 7-
tricarboxylic acid bismuth (1) is obtained. The high-purity large-scale preparation of the contrast agent can be realized, the synthetic
route is simple and controllable, and the product is high in water
solubility, low in
osmotic pressure, stable in property, high in safety and excellent in X-
ray imaging performance.