Improved process for synthesizing ioversol

A synthesis method and technology of ioversol are applied in the improved synthesis field of ioversol, can solve the problems such as inability to meet the needs of industrial production, difficulty in recovering solvent, etc., and achieve the effects of low cost, easy recovery of solvent and mild reaction conditions
CN100344609CInactive Publication Date: 2007-10-24JIANGSU INST OF NUCLEAR MEDICINE

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
JIANGSU INST OF NUCLEAR MEDICINE
Publication Date
2007-10-24
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides an improved method for synthesizing Ioversol, belonging to technology preparing non-ionic X contrast agent. The invention employs 5- hydroxyethyl amido- N, N' - (2,3-dihydroxy propyl)- 2, 4, 6- triiodide-1, 3- benezene diformamide and 2- chlorethanol to proceed nitrogen alkylation reaction in mixing solution of caustic soda and acetonitrile, neutralizing, desalting and desalting reacting solution, re-crystallizing with methyl glycol single dimethyl ether, and getting Ioversol. The invention is characterized by soft reacting condition, short reaction time, and stable quality, low cost and suitable for industrialized production.
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Description

technical field

[0001] The invention relates to an improved synthesis method of ioversol. The compound is a non-ionic X-ray contrast agent, which is suitable for CT examination, arteriovenous contrast and urography, etc., and belongs to the preparation technology of the non-ionic X-ray contrast agent. Background technique

[0002] Ioversol, the chemical name is N,N'-bis(2,3-dihydroxypropyl)-5-[N-(2-hydroxyethyl)-glycolamide]-2,4,6-tri Iodine-1,3-phthalamide, the trade name of its preparation is Anxili, structural formula (I):

[0003]

[0004] Ioversol has the advantages of large water solubility, low viscosity, low osmotic pressure, and low incidence of adverse reactions. Its preparation, Ioversol Injection, is widely used clinically for cardiovascular angiography and intravenous digital subtraction angiography.

[0005] U.S. Patent No. 4,396,598 discloses a synthetic technique of ioversol, the last step reaction of which is 5-hydroxyacetamido-N, N'-bis(2,3-dihydroxypro...

Claims

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