A new bismuth-based chelate ct contrast agent and its preparation method and application

By using a six-step reaction route to prepare bismuth(III)2,2',2''-(3,6,9-triazine-1(2,6)-pyridine-cyclodecane-3,6,9-triyl)tricarboxylic acid, the problems of X-ray attenuation capability and safety of existing CT contrast agents were solved, and the laboratory-scale preparation and clinical application of efficient and safe bismuth-based chelate CT contrast agents were realized.

CN121717810BActive Publication Date: 2026-06-23TIANJIN MEDICAL UNIV
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Patent Information

Application Number
CN202610221810.2
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2026-02-25
Publication Date
2026-06-23
Estimated Expiration
2046-02-25

AI Technical Summary

Technical Problem

Existing iodine-based CT contrast agents have limited X-ray attenuation capabilities, low imaging sensitivity, and safety issues such as kidney damage and iodine allergy. Non-ionic bismuth-based chelate CT contrast agents have low water solubility, making it difficult to balance water solubility, osmotic pressure, and stability, thus limiting their clinical application.

Method used

A novel bismuth-based chelate CT contrast agent was developed. The stable non-ionic small molecule chelate was synthesized through a six-step reaction using a method that utilizes bismuth(III)2,2',2''-(3,6,9-triazine-1(2,6)-pyridine-cyclodecane-3,6,9-triyl)tricarboxylic acid. A metal scavenger was added, a physiological buffer system was constructed, and the pH and stability of the solution were controlled, making it suitable for intravenous administration.

Benefits of technology

The laboratory-scale preparation of a bismuth-based chelate CT contrast agent with high X-ray attenuation capability has been achieved. It has low osmotic pressure, high water solubility and high stability, which reduces osmotic pressure stimulation during injection, improves biosafety and imaging effect, and is suitable for CT imaging of the digestive, urinary and circulatory systems.

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Abstract

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.
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