The application discloses a novel
bismuth-based chelate CT contrast agent and a preparation method and application thereof. The synthesis method comprises the following steps: 2,6-
pyridine dimethyl
alcohol is reacted with chlorosulfoxide to obtain 2,6-bis(chloromethyl)
pyridine; the 2,6-bis(chloromethyl)
pyridine is reacted with N,N',N''-
tris(p-tolylsulfonyl)divinyltriamine and an inorganic base in a
solvent and is heated, is deprotected by concentrated
sulfuric acid to obtain an intermediate pyclen; the pyclen is heated and reacted with a halogenated
carboxylic acid ester under alkaline conditions in a polar
organic solvent, is hydrolyzed to obtain a ligand product; and the ligand product is heated and chelated with a
bismuth agent to obtain the target
bismuth-based chelate. The application realizes the
laboratory scale preparation of the small-molecule bismuth-based chelate CT contrast agent, and a non-ionic contrast agent is prepared, which has low
osmotic pressure, high stability, high water
solubility and good
biological safety and is used for
CT imaging of the digestive
system, the
urinary system and the
circulatory system.