- Preparation method and intermediates of iopromide
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The present invention relates to a preparation method and intermediates of iopromide. The method specifically comprises: adopting a compound represented by a formula II as a starting raw material, and sequentially carrying out an acylation reaction, a lactonization reaction, a further acylation reaction, a reduction reaction, an iodination reaction, a re-acylation reaction and a final hydrolysis reaction to obtain the iopromide represented by a formula I, wherein a compound represented by a formula VII and a compound represented by a formula V are introduced as the intermediates so as to avoid the generation of the bismer by-product, the lactone ring is not easily subjected to ring opening removing during the iodination reaction process, and the introduced intermediates are easy to separate and purify, such that the high-purity iopromide can be prepared in the high-yield manner.
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Paragraph 0092; 0093; 0094
(2017/02/24)
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- Preparation technology of iopromide intermediate
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The invention provides an iopromide intermediate. A preparation technology of a compound 3-(2,3-dihydroxypropyl formamyl)-5-nitroisophthalic acid comprises the steps that monomethyl 5-nitroisophthalate is reacted with 3-amino propane-1,2-diol in alcohol solvent at appropriate heating temperature on the condition that strong alkali exists to obtain a product, wherein the reaction equation is shown in the specification. According to the preparation technology of the iopromide intermediate, the synthetic technology is good in selectivity, the synthetic route is simple, the product can be obtained through simple filtration, and the yield is high. Therefore, the technology has the advantages of being efficient, rapid and low in cost.
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- Synthesis of N1,N3-BIS(2,3-DIHYDROXYPROPYL)-5-NITROISOPHTHALAMIDE
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The present disclosure generally relates to a new process for the preparation of high purity 5-nitro-isophthalamide compounds, which are useful as intermediates for the preparation of imaging agents, such as iodinated x-ray contrast imaging agents like ioversol, iohexyl and iopamidol.
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Paragraph 0037-0038
(2014/07/23)
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- New brominated compounds as contrast media for X-ray mammography
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The invention regards new brominated compounds containing one or two phenyl rings with favorable physico-chemical properties, good tolerance profile, stability and suitable pharmacokinetic profile as contrast media for X-ray mammography, their pharmaceutical formulations and radiological application. The described new bromine contrast media will increase the sensitivity and specificity of X-ray mammography especially in problematic cases. The new contrast media have a higher X-ray absorption than iodine in the energy range used by mammography, a high hydrophilicity, lower toxicity and better tolerance profile than corresponding iodinated compounds.
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- Carboxamide non-ionic contrast media
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Novel triiodo 5-aminoisophthaldiamides are provided, where the amino and one of the amide nitrogens are substituted. The compounds have at least two hydroxyl groups and are found to provide low viscosity and osmolality. Procedures for preparing the compounds are provided.
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- Dicarboxylic acid-bis(3,5-dicarbamoyl-2,4,6-triiodoanilides) and x-ray contrast media containing them
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Dicarboxylic acid bis-(3,5-dicarbomoyl-2,4,6-triiodoanilides) of general formula I STR1 wherein the amide radicals --CONR1 R2 and --CONR3 R4 are different from one another and R1 is a hydrogen, a lower alkyl radical or R2, R2 is a straight-chain or branched-chain monohydroxy or polyhydroxy alkyl radical, R3 is hydrogen, a lower alkyl radical or R4, R4 is a straight-chain or branched-chain monohydroxy or polyhydroxy alkyl radical, R5 is hydrogen, a lower alkyl radical or a monohydroxy or polyhydroxy alkyl radical, X is a straight-chain or branched-chain alkylene with 1 to 6 carbon atoms, which optionally can be substituted by 1 to 6 hydroxy or alkoxy groups or interrupted by one or more oxygen atoms, possess good pharmacological and physicochemical properties rendering them outstandingly suitable as radiopaque substances in X-ray contrast media for use in all fields of application for X-ray contrast media.
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