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A New Contrast Agent of Triiodobenzene Compounds

The technology of a compound and a contrast agent is applied in the field of triiodobenzene compound and a contrast agent containing the compound, 5--N, and can solve the problems of high viscosity, toxicity and hypertonicity, etc.

Active Publication Date: 2011-12-14
ZHEJIANG STARRY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Clinical studies have found that the above-mentioned three types of iodine contrast agents all have one or another disadvantage, such as toxicity, hyperosmolarity, or high viscosity [Journal of West China Pharmaceutical Sciences, 2000, 15(1): 53-54]

Method used

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  • A New Contrast Agent of Triiodobenzene Compounds
  • A New Contrast Agent of Triiodobenzene Compounds
  • A New Contrast Agent of Triiodobenzene Compounds

Examples

Experimental program
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Effect test

Embodiment 15

[0026] Example 15-(N-methylacetylamino)-N, N'-bis(2,3-dihydroxy-n-propyl)-2,4,6-triiodoisophthalamide (I)

[0027]

[0028] Under ice-water bath cooling and mechanical stirring, 5-(acetylamino)-N,N'-bis(2,3-dihydroxy-n-propyl)-2,4,6-triiodoisophthalamide (I) (2000g , 2.677mol) (produced by Zhejiang Stellite Pharmaceutical Co., Ltd.), sodium hydroxide (139.2g, 3.480mol) was dissolved in 50% ethylene glycol monomethyl ether aqueous solution, stirred at room temperature, added methyl iodide (380.1g, 2.677mol), TLC followed the reaction process, and the reaction was completed in 6h. Concentrate under reduced pressure and use resin to purify and separate. The specific method is: prepare 5 liters of macroporous adsorption resin regenerated with 40% methanol, pack it into a glass column with a diameter of 100mm, pour the product aqueous solution into it, and let it absorb statically. For more than two hours, gradient elution was carried out with different concentrations of methan...

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Abstract

The invention relates to a novel contrast medium for a triiodobenzene compound and also provides a preparation method of the compound. The triiodobenzene compound is 5-(N-methylacetamide)-N,N'-di(2.3-dyhydroxy n-propyl)-2,4,6-triiodo isophthalamide (I) and has a structural formula shown as the specification.

Description

Technical field: [0001] The invention belongs to the field of non-ionic X-ray contrast agents, and relates to a triiodobenzene compound with excellent physical and chemical properties and a contrast agent containing the compound. More specifically, the compound of the present invention is 5-(N-methylacetamido)-N,N'-bis(2,3-dihydroxy-n-propyl)-2,4,6-triiodoisophthalamide . Background technique: [0002] Since the advent of diatrizoic acid (the first iodine contrast agent) in the 1950s, more than ten kinds of iodine contrast agents have been widely used in clinic as diagnostic reagents. It is reported that there are about 50 million patients who use contrast medium every year in the world [Curr. Opin. Allergy Clin Immunol, 2002(2): 333-339]. According to the permeability, this type of contrast agent can be divided into the following three categories: the first category is hypertonic iodine contrast agent, such as diatrizoic acid, diatrizoate meglumine, etc., and its osmotic ...

Claims

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Application Information

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IPC IPC(8): C07C237/46C07C231/12A61K49/04
Inventor 王哲张婷婷徐静静赵岳定林勇利沈伟艺熊安伟陈仕洪
Owner ZHEJIANG STARRY PHARMA